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Showing papers on "Solid lipid nanoparticle published in 2022"


Journal ArticleDOI
TL;DR: In this paper , the authors provide an overview about the different barriers for oral peptide and protein delivery, highlight the progress made on lipid-based nanocarriers in order to overcome them and discuss strengths and weaknesses of these delivery systems in comparison to other technologies.

72 citations


Journal ArticleDOI
TL;DR: Conventional methods and the rationale for large-scale production ofSolid lipid nanoparticles are discussed, including high-pressure homogenization (HPH), hot melt extrusion coupled with HPH, microchannels, nanoprecipitation using static mixers, and microemulsion-based methods.
Abstract: Solid lipid nanoparticles (SLNs) are an alternate carrier system to liposomes, polymeric nanoparticles, and inorganic carriers. SLNs have attracted increasing attention in recent years for delivering drugs, nucleic acids, proteins, peptides, nutraceuticals, and cosmetics. These nanocarriers have attracted industrial attention due to their ease of preparation, physicochemical stability, and scalability. These characteristics make SLNs attractive for manufacture on a large scale. Currently, several products with SLNs are in clinical trials, and there is a high possibility that SLN carriers will quickly increase their presence in the market. A large-scale manufacturing unit is required for commercial applications to prepare enough formulations for clinical studies. Furthermore, continuous processing is becoming more popular in the pharmaceutical sector to reduce product batch-to-batch differences. This review paper discusses some conventional methods and the rationale for large-scale production. It further covers recent progress in scale-up methods for the synthesis of SLNs, including high-pressure homogenization (HPH), hot melt extrusion coupled with HPH, microchannels, nanoprecipitation using static mixers, and microemulsion-based methods. These scale-up technologies enable the possibility of commercialization of SLNs. Furthermore, ongoing studies indicate that these technologies will eventually reach the pharmaceutical market.

35 citations


Journal ArticleDOI
TL;DR: Despite the development of curcumin‐containing NPs for the treatment of cancer, potentially serious side effects, including interactions with other drugs, some toxicity aspects of NPs may occur that require more high‐quality investigations to firmly establish the clinical efficacy.
Abstract: Curcumin is a phytochemical achieved from the plant turmeric. It is extensively utilized for the treatment of several types of diseases such as cancers. Nevertheless, its efficiency has been limited because of rapid metabolism, low bioavailability, poor water solubility, and systemic elimination. Scientists have tried to solve these problems by exploring novel drug delivery systems such as lipid‐based nanoparticles (NPs) (e.g., solid lipid NPs, nanostructured lipid carriers, and liposomes), polymeric NPs, micelles, nanogels, cyclodextrin, gold, and mesoporous silica NPs. Among these, liposomes have been the most expansively studied. This review mainly focuses on the different curcumin nanoformulations and their use in cancer therapy in vitro, in vivo, and clinical studies. Despite the development of curcumin‐containing NPs for the treatment of cancer, potentially serious side effects, including interactions with other drugs, some toxicity aspects of NPs may occur that require more high‐quality investigations to firmly establish the clinical efficacy.

33 citations


Journal ArticleDOI
TL;DR: A review of the state-of-the-art related to the synthesis and applications of popular nanoparticles in medicine, with a focus on their use, e.g., in COVID-19 vaccines is presented in this paper .
Abstract: Currently, carriers of active ingredients in the form of particles of a size measured in nanometers are the focus of interest of research centers worldwide. So far, submicrometer emulsions, liposomes, as well as microspheres, and nanospheres made of biodegradable polymers have been used in medicine. Recent studies show particular interest in nanoparticles based on lipids, and at the present time, are even referred to as the “era of lipid carriers”. With the passage of time, lipid nanoparticles of the so-called first and second generation, SLN (Solid Lipid Nanoparticles) and nanostructured lipid carriers and NLC (Nanostructured Lipid Carriers), respectively, turned out to be an alternative for all imperfections of earlier carriers. These carriers are characterized by a number of beneficial functional properties, including, among others, structure based on lipids well tolerated by the human body, high stability, and ability to carry hydro- and lipophilic compounds. Additionally, these carriers can enhance the distribution of the drug in the target organ and alter the pharmacokinetic properties of the drug carriers to enhance the medical effect and minimize adverse side effects. This work is focused on the current review of the state-of-the-art related to the synthesis and applications of popular nanoparticles in medicine, with a focus on their use, e.g., in COVID-19 vaccines.

28 citations


Journal ArticleDOI
01 Feb 2022-Heliyon
TL;DR: In this article , the physicochemical and biopharmaceutical aspects encountered in the pathway of drugs through the skin, and the potential added value of using solid lipid nanoparticles (SLN) and nanostructured lipid vectors (NLC) to drug permeation/penetration through this route.

25 citations


Journal ArticleDOI
TL;DR: Functionalization approaches to overcome the drawbacks of lipid nanoparticles, as well as the exploration of new functional additives with the potential to improve the penetration of macromolecular pharmaceuticals, would quickly progress the challenging field of ocular drug delivery systems.
Abstract: Due to complicated anatomical and physical properties, targeted drug delivery to ocular tissues continues to be a key challenge for formulation scientists. Various attempts are currently being made to improve the in vivo performance of therapeutic molecules by encapsulating them in various nanocarrier systems or devices and administering them via invasive/non-invasive or minimally invasive drug administration methods. Biocompatible and biodegradable lipid nanoparticles have emerged as a potential alternative to conventional ocular drug delivery systems to overcome various ocular barriers. Lipid-based nanocarrier systems led to major technological advancements and therapeutic advantages during the last few decades of ocular therapy, such as high precorneal residence time, sustained drug release profile, minimum dosing frequency, decreased drug toxicity, targeted site delivery, and, therefore, an improvement in ocular bioavailability. In addition, such formulations can be given as fine dispersion in patient-friendly droppable preparation without causing blurred vision and ocular sensitivity reactions. The unique advantages of lipid nanoparticles, namely, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and liposomes in intraocular targeted administration of various therapeutic drugs are extensively discussed. Ongoing and completed clinical trials of various liposome-based formulations and various characterization techniques designed for nanoemulsion in ocular delivery are tabulated. This review also describes diverse solid lipid nanoparticle preparation methods, procedures, advantages, and limitations. Functionalization approaches to overcome the drawbacks of lipid nanoparticles, as well as the exploration of new functional additives with the potential to improve the penetration of macromolecular pharmaceuticals, would quickly progress the challenging field of ocular drug delivery systems.

23 citations


Journal ArticleDOI
TL;DR: In this paper , the effect of utilizing lipidic nanoparticles is discussed as well as the different tumor uptake enhancement techniques used in treating hepatocellular carcinoma, which is considered to be the most common type of liver cancer.
Abstract: Liver cancer is considered one of the deadliest diseases with one of the highest disease burdens worldwide. Among the different types of liver cancer, hepatocellular carcinoma is considered to be the most common type. Multiple conventional approaches are being used in treating hepatocellular carcinoma. Focusing on drug treatment, regular agents in conventional forms fail to achieve the intended clinical outcomes. In order to improve the treatment outcomes, utilizing nanoparticles-specifically lipid based nanoparticles-are considered to be one of the most promising approaches being set in motion. Multiple forms of lipid based nanoparticles exist including liposomes, solid lipid nanoparticles, nanostructured lipid carriers, microemulsion, nanoemulsion, phytosomes, lipid coated nanoparticles, and nanoassemblies. Multiple approaches are used to enhance the tumor uptake as well tumor specificity such as intratumoral injection, passive targeting, active targeting, and stimuli responsive nanoparticles. In this review, the effect of utilizing lipidic nanoparticles is being discussed as well as the different tumor uptake enhancement techniques used.

22 citations


Journal ArticleDOI
TL;DR: The efficacies and brain targeting efficiencies of these formulations based on considerations of their pharmacokinetic parameters and toxicities are discussed, some gaps in current knowledge are pointed out, and future developmental targets are proposed.
Abstract: Nose-to-brain drug delivery has been of great interest for the treatment of many central nervous system (CNS) diseases and psychiatric disorders over past decades. Several nasally administered formulations have been developed to circumvent the blood-brain barrier and directly deliver drugs to the CNS through the olfactory and trigeminal pathways. However, the nasal mucosa’s drug absorption is insufficient and the volume of the nasal cavity is small, which, in combination, make nose-to-brain drug delivery challenging. These problems could be minimized using formulations based on solid lipid nanoparticles (SLNs) or nanostructured lipid carriers (NLCs), which are effective nose-to-brain drug delivery systems that improve drug bioavailability by increasing drug solubility and permeation, extending drug action, and reducing enzymatic degradation. Various research groups have reported in vivo pharmacokinetics and pharmacodynamics of SLNs and NLCs nose-to-brain delivery systems. This review was undertaken to provide an overview of these studies and highlight research performed on SLN and NLC-based formulations aimed at improving the treatment of CNS diseases such neurodegenerative diseases, epilepsy, and schizophrenia. We discuss the efficacies and brain targeting efficiencies of these formulations based on considerations of their pharmacokinetic parameters and toxicities, point out some gaps in current knowledge, and propose future developmental targets.

22 citations


Journal ArticleDOI
TL;DR: In this article , a review highlights recent studies on nanocarries used as delivery systems for DL including polymeric nanoparticles, micelles, nanoliposomes, solid lipid nanoparticles and nanosuspensions for DL.

21 citations


Journal ArticleDOI
TL;DR: In this paper , solid lipid nanoparticles (SLNs) were used as a drug delivery system to improve the dissolution, absorption and bioavailability of Cilostazol (CLZ).

21 citations


Journal ArticleDOI
TL;DR: In this article , a mucoadhesive buccal tablet containing LRX -loaded solid lipid nanoparticles (SLNs) was developed to enhance the drug solubility and bioavailability and achieve a controlled release pattern for a better anti-inflammatory effect.

Journal ArticleDOI
TL;DR: A comprehensive review of various quercetin nano-formulations developed last decade for topical delivery is presented in this paper , where the relevant literature was collected from an exhaustive search on databases like PubMed, ScienceDirect, Google Scholar, and others using various keywords, including “quercetoin nanoformulations,” “dermal nanoformulation of querceto-benzmann et al.,” and many others.
Abstract: Quercetin is one of the most critical endogenous anti-oxidants used widely in cosmetics, nutraceuticals, and pharmaceuticals products for skincare and therapeutics due to its protective character against oxidants and inflammation. Although low hydrophilicity and poor percutaneous absorption of quercetin make it an untrustworthy entrant for topical delivery, numerous new perspectives have been developed and proposed to overwhelm these problems. Amongst multiple outlooks, nanoparticles-based drug delivery system has gained highlighted attention and showed various advantages in topical delivering a hydrophobic drug like quercetin. The relevant literature was collected from an exhaustive search on databases like PubMed, ScienceDirect, Google Scholar, and others using various keywords, including “quercetin nanoformulations,” “dermal nanoformulations of quercetin,” “quercetin topical formulations,” and many others. Publications in the English language accessed till July 2021 were chosen, whereas non-English language papers, dissertations, unpublished data, and non-original papers were excluded from the study. The present review comprises of various quercetin nanoformulations developed last decade for topical delivery of quercetin. Until recently, numerous nanocarriers systems, including nanovesicles, nanospheres, nanocapsules, nanogels, nanofibres, nanoemulsions, micelles, gold nanoparticles, silica nanoparticles, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs), have been developed for skin delivery of quercetin that not only improves the solubility and skin permeability but also augments the physicochemical stability and provides sustain and control release. Nanostructured particles of herbal drugs offer several advantages over other conventional drug delivery systems. Advanced delivery formulations not only help in solving hitches such as poor solubility, bioavailability and stability of quercetin, but also, in the case of topical delivery, overcome the formidable barrier of the skin. Indeed, the application of herbal nanomedicine and herbal nano-drug delivery system is certainly the trend. However, for clinical utilization of such formulations, their investigation in humans needs to be explored. Such exploration along with in depth analysis and dose optimization can pave way for commercial success of quercetin advanced carrier systems for topical application.

Journal ArticleDOI
TL;DR: In this article , the authors examined the current status of nano-encapsulation of food, and deemed further synthesis regards the aspects applied to (food) bioactive constituents needful, and revisited how nano encapsulation delivers and same time protects the bioactivity of nutrients, nutraceuticals, and other food constituents.

Journal ArticleDOI
TL;DR: A review of the state of the art on the use of lipid nanoparticles to modify the pharmacokinetics of drugs employed in the management of neurological disorders can be found in this article .

Journal ArticleDOI
TL;DR: The study provided a theoretical basis for the use of novel microneedle containing curcumin-loaded solid lipid nanoparticles as a useful tool for the treatment of Parkinson’s disease.
Abstract: Curcumin is well known for its neuroprotective effect, and also able to alleviate Parkinsonian features. Clinical application of curcumin is limited due to its low bioavailability. Hence, we hypothesized that the microneedles (MN) containing drug-loaded solid lipid nanoparticles (SLNs) may be able to improve its bioavailability and efficacy. The SLNs were prepared with microemulsion technique using glyceryl monostearate as a lipid and tween 80 as a stabilizer. The particle size, polydispersity index, zeta potential, and entrapment efficiency of prepared SLNs were determined. The optimized formulation was incorporated into microneedle arrays using micromolding technique and fabricated microneedle patch were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, optical microscopy, ex vivo permeation studies, histology studies, and fluorescent microscopy. The fabricated microneedle patch was also evaluated for neuroprotective activity and skin irritation potential. Fourier transform infrared spectroscopy studies of SLNs and microneedles confirmed the chemical compatibility of excipients with curcumin. The developed microneedles were also found to be non-irritant with decreased degree of bradykinesia, high motor coordination, and balance ability. The study provided a theoretical basis for the use of novel microneedle containing curcumin-loaded solid lipid nanoparticles as a useful tool for the treatment of Parkinson’s disease.

Journal ArticleDOI
TL;DR: The easy and simple scalability of novel SLNs and nano lipid carriers, along with their various processing procedures, recent developments, limitation and toxicity, formulation optimization and approaches for the manufacture of lipid nanoparticles, lyophilization and drug release are comprehensively discussed in this review.
Abstract: Abstract The bioavailability of drugs is dependent on several factors such as solubility and the administration route. A drug with poor aqueous solubility, therefore, poses challenges with regards to its pharmaceutical advance and ultimately its biological usage. Lipid nanoparticles have been used in pharmaceutical science due to their importance in green chemistry. Their biochemical properties as ‘green’ materials and biochemical processes as ‘green’ processes mean they can be environmentally sustainable. Generally, lipid nanoparticles can be employed as carriers for both lipophilic and hydrophilic drugs. The proposed administration route for nanoparticles can present advantages and disadvantages which should be considered by a formulator. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are attractive delivery systems because of their ease of manufacture, biocompatibility, biodegradability, and scale-up capacity of formulation constituents. The easy and simple scalability of novel SLNs and nano lipid carriers, along with their various processing procedures, recent developments, limitation and toxicity, formulation optimization and approaches for the manufacture of lipid nanoparticles, lyophilization and drug release are comprehensively discussed in this review. This review also summarizes the research data related to the various preparation methods and excipients used for SLNs and NLCs in recent years.

Journal ArticleDOI
TL;DR: In this work, closed-loop high-pressure homogenization was used for the first time and compared to the currently preferred open-loop method.
Abstract: Solid lipid nanoparticles (SLNs) have been synthesized as potential drug delivery systems. They are classified as solid lipid nanocarriers that can successfully carry both hydrophilic and hydrophobic drugs. SLNs are based on a biocompatible lipid matrix that is enzymatically degraded into natural components found in the human body. Solid lipid nanoparticles are suitable for the incorporation of hydrophobic active ingredients such as curcumin. The study included the optimization of lipid nanoparticle composition, incorporation of the active compound (curcumin), a stability evaluation of the obtained nanocarriers and characterization of their lipid matrix. Through process optimization, a dispersion of solid lipid nanoparticles (solid lipid:surfactant—2:1.25 weight ratio) predisposed to the incorporation of curcumin was developed. The encapsulation efficiency of the active ingredient was determined to be 99.80%. In stability studies, it was found that the most suitable conditions for conducting high-pressure homogenization are 300 bar pressure, three cycles and a closed-loop system. This yields the required values of the physicochemical parameters (a particle size within a 200–450 nm range; a polydispersity index of <30%; and a zeta potential of about |±30 mV|). In this work, closed-loop high-pressure homogenization was used for the first time and compared to the currently preferred open-loop method.

Journal ArticleDOI
TL;DR: In this article , the microneedles (MN) containing drug-loaded solid lipid nanoparticles (SLNs) may be able to improve its bioavailability and efficacy for the treatment of Parkinson's disease.
Abstract: Curcumin is well known for its neuroprotective effect, and also able to alleviate Parkinsonian features. Clinical application of curcumin is limited due to its low bioavailability. Hence, we hypothesized that the microneedles (MN) containing drug-loaded solid lipid nanoparticles (SLNs) may be able to improve its bioavailability and efficacy. The SLNs were prepared with microemulsion technique using glyceryl monostearate as a lipid and tween 80 as a stabilizer. The particle size, polydispersity index, zeta potential, and entrapment efficiency of prepared SLNs were determined. The optimized formulation was incorporated into microneedle arrays using micromolding technique and fabricated microneedle patch were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, optical microscopy, ex vivo permeation studies, histology studies, and fluorescent microscopy. The fabricated microneedle patch was also evaluated for neuroprotective activity and skin irritation potential. Fourier transform infrared spectroscopy studies of SLNs and microneedles confirmed the chemical compatibility of excipients with curcumin. The developed microneedles were also found to be non-irritant with decreased degree of bradykinesia, high motor coordination, and balance ability. The study provided a theoretical basis for the use of novel microneedle containing curcumin-loaded solid lipid nanoparticles as a useful tool for the treatment of Parkinson’s disease.

Journal ArticleDOI
26 Jan 2022-Cancers
TL;DR: This comprehensive review discusses the preparation and targeting techniques as well as the properties of several liposome-, micelle-, solid-lipid nanoparticle-, dendrimer-, gold-, and magnetic-nanoparticle-based delivery systems for anticancer drugs.
Abstract: Simple Summary The current main technological strategies for the delivery of anticancer drugs are discussed herein. This comprehensive review may help researchers design suitable delivery systems. Abstract Several drug-delivery systems have been reported on and often successfully applied in cancer therapy. Cell-targeted delivery can reduce the overall toxicity of cytotoxic drugs and increase their effectiveness and selectivity. Besides traditional liposomal and micellar formulations, various nanocarrier systems have recently become the focus of developmental interest. This review discusses the preparation and targeting techniques as well as the properties of several liposome-, micelle-, solid-lipid nanoparticle-, dendrimer-, gold-, and magnetic-nanoparticle-based delivery systems. Approaches for targeted drug delivery and systems for drug release under a range of stimuli are also discussed.

Journal ArticleDOI
01 Jan 2022
TL;DR: In this paper , the authors attempted to recount the unique features of emerging platforms of nano-carriers, which are corresponding to the lycopene loading and controlled delivery, and extended the innovative progress in nanoencapsulation of Lycopene with an emphasis on the factors influencing its bioaccessibility in such nanovehicles, together with their shortcomings and upcoming evolutions.
Abstract: Lycopene, as a promising biofunctional ingredient in human diet, is attaining huge importance nowadays. Besides its critical importance as a natural colorant, more especially, it is considered as a health-promotional component that endows a multitude of advantageous features. Nonetheless, its inefficiency vs. process/environmental stresses, poor-aqueous solubility, plus poor-bioavailability are the most bottlenecks limiting food/pharma utilization. At the same time, the field of nano-dimensional bioactive delivery vehicles has developed quickly. In this scenario, the most prominent instances of such carriers are lipid-based nanoformulations (i.e., nano-/Pickering/double emulsions, surfactant-based nano-vectors, nano-structured lipid carriers (NLCs), solid lipid nano-particles (SLNs), etc.) and biopolymeric nano-structures (e.g., nano-hydrogels/organogels/oleogels, nanofibers, nanotubes, cyclodextrins, and protein-polysaccharide nanocomplexes/conjugates). To take benefit of these properties, a foundational understanding of why lycopene nanodelivery systems are such unbeatable nano-systems and how we could utilize their potentials is crucial. Here, we attempted to recount the unique features of emerging platforms of nano-carriers, which are corresponding to the lycopene loading and controlled delivery. Discussion was also extended to cover the innovative progress in nanoencapsulation of lycopene with an emphasis on the factors influencing its bioaccessibility in such nanovehicles, together with their shortcomings and upcoming evolutions. Biopolymeric and lipid-based nano-structures, as attractive and effectual nanovehicles, have demonstrated to be potential strategies for the protection of lycopene throughout the digestive system along with representing an efficacious targeted release.

Journal ArticleDOI
TL;DR: PC-SLNs can greatly reduce the dose of PTX while still achieving the same therapeutic effect on four cancer cell lines, among which the inhibitory effect on A549 lung cancer cells was the strongest.
Abstract: Abstract The main aim of this study was to improve the therapeutic potential of a paclitaxel (PTX) and curcumin (CU) combination regimen using solid lipid nanoparticles (SLNs). PTX and CU were successfully co-encapsulated at a predetermined ratio in SLNs (PC-SLNs) with high encapsulation efficiency (CU: 97.6%, PTX: 95.8%), appropriate particle size (121.8 ± 1.69 nm), small PDI (0.267 ± 0.023), and negative zeta potential (–30.4 ± 1.25 mV). Compared with PTX or the combination of CU and PTX (CU + PTX), PC-SLNs can greatly reduce the dose of PTX while still achieving the same therapeutic effect on four cancer cell lines, among which the inhibitory effect on A549 lung cancer cells was the strongest. PC-SLNs improved the area under the curve (CU: 1.40-fold; PTX: 2.88-fold), prolonged the residence time (CU: 6.94-fold; PTX: 2.51-fold), and increased the half-life (CU: 5.62-fold; PTX: 6.46-fold), achieving long circulation. PC-SLNs were used to treat lung cancer in a nude mouse xenograft tumor model and the tumor suppression rate reached 78.42%, while those of PTX and (CU + PTX) were 40.53% and 51.56%, respectively. As PC-SLNs can prevent P-glycoprotein efflux, reverse MDR and downregulate the NF-κB pathway. PC-SLNs are a potential antineoplastic agent that is more effective and less toxic in treating lung cancer.

Journal ArticleDOI
TL;DR: The state of the art about different types of LNPs with the latest advances reported for the treatment of TNBC in recent years are compiled, along with their clinical status and toxicity in detail.
Abstract: Triple-negative breast cancer is considered the most aggressive type of breast cancer among women and the lack of expressed receptors has made treatment options substantially limited. Recently, various types of nanoparticles have emerged as a therapeutic option against TNBC, to elevate the therapeutic efficacy of the existing chemotherapeutics. Among the various nanoparticles, lipid-based nanoparticles (LNPs) viz. liposomes, nanoemulsions, solid lipid nanoparticles, nanostructured lipid nanocarriers, and lipid–polymer hybrid nanoparticles are developed for cancer treatment which is well confirmed and documented. LNPs include various therapeutic advantages as compared to conventional therapy and other nanoparticles, including increased loading capacity, enhanced temporal and thermal stability, decreased therapeutic dose and associated toxicity, and limited drug resistance. In addition to these, LNPs overcome physiological barriers which provide increased accumulation of therapeutics at the target site. Extensive efforts by the scientific community could make some of the liposomal formulations the clinical reality; however, the relatively high cost, problems in scaling up the formulations, and delivery in a more targetable fashion are some of the major issues that need to be addressed. In the present review, we have compiled the state of the art about different types of LNPs with the latest advances reported for the treatment of TNBC in recent years, along with their clinical status and toxicity in detail.

Journal ArticleDOI
TL;DR: In this paper , a combination of high shear homogenization and ultrasonic methods to load zeaxanthin and reduce its hydrophobicity was used to produce nano-based lipid carriers.

Journal ArticleDOI
TL;DR: Solid lipid nanoparticles, a class of colloidal drug carriers made of lipids, have emerged as potentially effective drug delivery systems and are associated with numerous advantages such as low toxicity, high bioavailability of drugs, versatility in the incorporation of hydrophilic and lipophilic drugs, and the potential for production of large quantities of the carrier systems.
Abstract: Combating multiple drug resistance necessitates the delivery of drug molecules at the cellular level. Novel drug delivery formulations have made it possible to improve the therapeutic effects of drugs and have opened up new possibilities for research. Solid lipid nanoparticles (SLNs), a class of colloidal drug carriers made of lipids, have emerged as potentially effective drug delivery systems. The use of SLNs is associated with numerous advantages such as low toxicity, high bioavailability of drugs, versatility in the incorporation of hydrophilic and lipophilic drugs, and the potential for production of large quantities of the carrier systems. The SLNs and nanostructured lipid carriers (NLCs) are the two most frequently used types of nanoparticles. These types of nanoparticles can be adjusted to deliver medications in specific dosages to specific tissues, while minimizing leakage and binding to non-target tissues.

Journal ArticleDOI
TL;DR: The anticancer activity of one formulation was extremely significant in all tested cancer cell lines at all incubation times, which is very promising.
Abstract: This work aimed to optimize a celecoxib (CXB)-loaded solid lipid nanoparticles (SLN) colon delivery system for the enhancement of anticancer activity. An ultrasonic melt-emulsification method was employed in this work for the preparation of SLN. The physical attributes were characterized for their particle sizes, charges, morphology, and entrapment efficiency (%EE), in addition to DSC and FTIR. The in vitro drug release profiles were evaluated, and the anticancer activity was examined utilizing an MTT assay in three cancer cell lines: the colon cancer HT29, medulloblastoma Daoy, and hepatocellular carcinoma HepG2 cells. All of the prepared SLN formulations had nanoscale particle sizes ranging from 238 nm to 757 nm. High zeta-potential values (mv) within −30 s mv were reported. The %EE was in the range 86.76–96.6%. The amorphous nature of the SLN-entrapped CXB was confirmed from SLN DSC thermograms. The in vitro release profile revealed a slow constant rate of release with no burst release, which is unusual for SLN. Both the F9 and F14 demonstrated almost complete CXB release within 24 h, with only 25% completed within the first 5 h. F9 caused a significant percentage of cell death in the three cancer cell lines tested after 24 h of incubation and maintained this effect for 72 h. The prepared CXB-loaded SLN exhibited unique properties such as slow release with no burst and a high %EE. The anticancer activity of one formulation was extremely significant in all tested cancer cell lines at all incubation times, which is very promising.

Journal ArticleDOI
01 Mar 2022-Methods
TL;DR: In this paper , the procedures involved in emulsification-solvent evaporation method, one of the commonly utilized methods for preparation of NLCs, are described in detail.

Journal ArticleDOI
TL;DR: In this paper , the phase inversion temperature (PIT) method was used to prepare nanoemulsions (NE) and solid lipid nanoparticles (SLN) for drug delivery.

Journal ArticleDOI
TL;DR: Results demonstrated that PTZ-loaded SLNs can improve the bioavailability of PTZ by bypassing the hepatic metabolism via the lymphatic uptake, for controlled and sustained drug delivery.
Abstract: Pentazocine (PTZ), a narcotic-antagonist analgesic, has been extensively used in the treatment of initial carcinogenic or postoperative pain. Hepatic first-pass metabolism results in low oral bioavailability and high dose wastage. Herein, 10 mg (-)-Pentazocine (HPLC-grade) was incorporated to solid lipid nanoparticles (SLNs) using a double water-oil-water (w/o/w) emulsion by solvent emulsification–evaporation technique, followed by high shear homogenization to augment its oral bioavailability, considering the lymphatic uptake. The resulting SLNs were characterized for zeta potential (ZP), particle size (PS), and polydispersity index (PDI) using a zetasizer. The entrapment efficiency (EE) and loading capacity (LC) were calculated. Chemical interactions, through the identification of active functional groups, were assessed by Fourier-transformed infrared (FTIR) spectroscopy. The nature (crystallinity) of the SLNs was determined by X-ray diffractometry (XRD). The surface morphology was depicted by transmission electron microscopy (TEM). In vitro (in Caco-2 cells) and in vivo (in male Wistar rats) investigations were carried out to evaluate the PTZ release behavior and stability, as well as the cellular permeation, cytotoxicity, systemic pharmacokinetics, antinociceptive, anti-inflammatory, and antioxidative activities of PTZ-loaded SLNs, mainly compared to free PTZ (marketed conventional dosage form). The optimized PTZ-loaded SLN2 showed significantly higher in vitro cellular permeation and negligible cytotoxicity. The in vivo bioavailability and pharmacokinetics parameters (t1/2, Cmax) of the PTZ-loaded SLNs were also significantly improved, and the nociception and inflammation, following carrageenan-induced inflammatory pain, were markedly reduced. Concordantly, PTZ-loaded SLNs showed drastic reduction in the oxidative stress (e.g., malonaldehyde (MDA)) and proinflammatory cytokines (e.g., Interleukin (IL)-1β, -6, and TNF-α). The histological features of the paw tissue following, carrageenan-induced inflammation, were significantly improved. Taken together, the results demonstrated that PTZ-loaded SLNs can improve the bioavailability of PTZ by bypassing the hepatic metabolism via the lymphatic uptake, for controlled and sustained drug delivery.

Journal ArticleDOI
TL;DR: A synthesis of the last ten years of research on nanodelivery systems used for the delivery of essential oils as well as their potential as a viable alternative to antibiotics in human and veterinary therapy is provided.
Abstract: Abstract This review provides a synthesis of the last ten years of research on nanodelivery systems used for the delivery of essential oils (EOs), as well as their potential as a viable alternative to antibiotics in human and veterinary therapy. The use of essential oils alone in therapy is not always possible due to several limitations but nanodelivery systems seem to be able to overcome these issues. The choice of the essential oil, as well as the choice of the nanodelivery system influences the therapeutic efficacy obtained. While several studies on the characterization of EOs exist, this review assesses the characteristics of the nanomaterials used for the delivery of essential oils, as well as impact on the functionality of nanodelivered essential oils, and successful applications. Two classes of delivery systems stand out: polymeric nanoparticles (NPs) including chitosan, cellulose, zein, sodium alginate, and poly(lactic-co-glycolic) acid (PLGA), and lipidic NPs including nanostructured lipid carriers, solid lipid NPs, nanoemulsions, liposomes, and niosomes. While the advantages and disadvantages of these delivery systems and information on stability, release, and efficacy of the nanodelivered EOs are covered in the literature as presented in this review, essential information, such as the speed of emergence of a potential bacteria resistance to these new systems, or dosages for each type of infection and for each animal species or humans is still missing today. Therefore, more quantitative and in vivo studies should be conducted before the adoption of EOs loaded NPs as an alternative to antibiotics, where appropriate.

Journal ArticleDOI
TL;DR: A comprehensive overview of the different structured edible lipid-based oral delivery systems investigated up to date can be found in this paper , which emphasizes the contribution of each system component to the delivery performance, and the oral delivery path of lipids.