Showing papers on "Solid lipid nanoparticle published in 2014"

Essential Oils Loaded in Nanosystems: A Developing Strategy for a Successful Therapeutic Approach

Abstract: Essential oils are complex blends of a variety of volatile molecules such as terpenoids, phenol-derived aromatic components, and aliphatic components having a strong interest in pharmaceutical, sanitary, cosmetic, agricultural, and food industries. Since the middle ages, essential oils have been widely used for bactericidal, virucidal, fungicidal, antiparasitical, insecticidal, and other medicinal properties such as analgesic, sedative, anti-inflammatory, spasmolytic, and locally anaesthetic remedies. In this review their nanoencapsulation in drug delivery systems has been proposed for their capability of decreasing volatility, improving the stability, water solubility, and efficacy of essential oil-based formulations, by maintenance of therapeutic efficacy. Two categories of nanocarriers can be proposed: polymeric nanoparticulate formulations, extensively studied with significant improvement of the essential oil antimicrobial activity, and lipid carriers, including liposomes, solid lipid nanoparticles, nanostructured lipid particles, and nano- and microemulsions. Furthermore, molecular complexes such as cyclodextrin inclusion complexes also represent a valid strategy to increase water solubility and stability and bioavailability and decrease volatility of essential oils.

Application of nanotechnology in improving bioavailability and bioactivity of diet-derived phytochemicals.

Abstract: Nanotechnology is an innovative approach that has potential applications in nutraceutical research. Phytochemicals have promising potential for maintaining and promoting health, as well as preventing and potentially treating some diseases. However, the generally low solubility, stability, bioavailability and target specificity, together with the side effects seen when used at high levels, have limited their application. Indeed, nanoparticles can increase solubility and stability of phytochemicals, enhance their absorption, protect them from premature degradation in the body and prolong their circulation time. Moreover, these nanoparticles exhibit high differential uptake efficiency in the target cells (or tissue) over normal cells (or tissue) through preventing them from prematurely interacting with the biological environment, enhanced permeation and retention effect in disease tissues and improving their cellular uptake, resulting in decreased toxicity, In this review, we outline the commonly used biocompatible and biodegradable nanoparticles including liposomes, emulsions, solid lipid nanoparticles, nanostructured lipid carriers, micelles and poly(lactic-co-glycolic acid) nanoparticles. We then summarize studies that have used these nanoparticles as carriers for epigallocatechin gallate, quercetin, resveratrol and curcumin administration to enhance their aqueous solubility, stability, bioavailability, target specificity and bioactivities.

Nanoparticle-Mediated Pulmonary Drug Delivery: A Review

Abstract: Colloidal drug delivery systems have been extensively investigated as drug carriers for the application of different drugs via different routes of administration. Systems, such as solid lipid nanoparticles, polymeric nanoparticles and liposomes, have been investigated for a long time for the treatment of various lung diseases. The pulmonary route, owing to a noninvasive method of drug administration, for both local and systemic delivery of an active pharmaceutical ingredient (API) forms an ideal environment for APIs acting on pulmonary diseases and disorders. Additionally, this route offers many advantages, such as a high surface area with rapid absorption due to high vascularization and circumvention of the first pass effect. Aerosolization or inhalation of colloidal systems is currently being extensively studied and has huge potential for targeted drug delivery in the treatment of various diseases. Furthermore, the surfactant-associated proteins present at the interface enhance the effect of these formulations by decreasing the surface tension and allowing the maximum effect. The most challenging part of developing a colloidal system for nebulization is to maintain the critical physicochemical parameters for successful inhalation. The following review focuses on the current status of different colloidal systems available for the treatment of various lung disorders along with their characterization. Additionally, different in vitro, ex vivo and in vivo cell models developed for the testing of these systems with studies involving cell culture analysis are also discussed.

Development and evaluation of lipid nanocarriers for quercetin delivery: A comparative study of solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and lipid nanoemulsions (LNE)

Abstract: To understand the effect of the physical state and composition of the lipid materials on the formation and performance of lipid nanocarriers, three types of carriers namely, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and lipid nanoemulsions (LNE) were prepared and compared. Quercetin was used as a model nutraceutical compound to evaluate the potency of these nanocarriers to increase bioaccessibility. Among the developed nanocarriers, quercetin loaded and free NLC showed the smallest particle size (∼34 and 47 nm) compared to SLN (∼103 and 127 nm) and LNE (∼82 and 83 nm). Encapsulation efficiency of quercetin in these nanocarriers was >90%. Stability of these nanocarriers in simulated stomach conditions was proved by their unaffected size and size distribution after incubation in simulated gastric fluid. Maximum bioaccessibility was observed with NLC and LNE (∼60%) compared to SLN (∼35%) and free quercetin solution (∼7%). Controlled release was observed in enzyme free simulated intestinal fluid with maximum release being obtained with LNE compared to SLN and NLC. This study showed that by optimally controlling the lipid physical state and composition, it is possible to fabricate the lipid nanocarriers with desired properties.

Delivery of Lipophilic Bioactives: Assembly, Disassembly, and Reassembly of Lipid Nanoparticles

Abstract: The oral bioavailability of lipophilic bioactive molecules can be greatly increased by encapsulating them within engineered lipid nanoparticles (ELNs), such as micelles, microemulsions, nanoemulsions, or solid lipid nanoparticles (SLNs). After ingestion, these ELNs are disassembled in the gastrointestinal tract (GIT) and then reassembled into biological lipid nanoparticles (mixed micelles) in the small intestine. These mixed micelles solubilize and transport lipophilic bioactive components to the epithelial cells. The mixed micelles are then disassembled and reassembled into yet another form of biological lipid nanoparticle [chylomicrons (CMs)] within the enterocyte cells. The CMs carry the bioactive components into the systemic (blood) circulation via the lymphatic system, thereby avoiding first-pass metabolism. This article provides an overview of the various physicochemical and physiological processes responsible for the assembly and disassembly of lipid nanoparticles outside and inside the GIT. This knowledge can be used to design food-grade delivery systems to improve the oral bioavailability of encapsulated lipophilic bioactive components.

Cubic and Hexagonal Liquid Crystals as Drug Delivery Systems

Abstract: Lipids have been widely used as main constituents in various drug delivery systems, such as liposomes, solid lipid nanoparticles, nanostructured lipid carriers, and lipid-based lyotropic liquid crystals. Among them, lipid-based lyotropic liquid crystals have highly ordered, thermodynamically stable internal nanostructure, thereby offering the potential as a sustained drug release matrix. The intricate nanostructures of the cubic phase and hexagonal phase have been shown to provide diffusion controlled release of active pharmaceutical ingredients with a wide range of molecular weights and polarities. In addition, the biodegradable and biocompatible nature of lipids demonstrates the minimum toxicity and thus they are used for various routes of administration. Therefore, the research on lipid-based lyotropic liquid crystalline phases has attracted a lot of attention in recent years. This review will provide an overview of the lipids used to prepare cubic phase and hexagonal phase at physiological temperature, as well as the influencing factors on the phase transition of liquid crystals. In particular, the most current research progresses on cubic and hexagonal phases as drug delivery systems will be discussed.

Compritol 888 ATO: a multifunctional lipid excipient in drug delivery systems and nanopharmaceuticals

Abstract: Introduction: Compritol® 888 ATO is a lipid excipient that is generally used in cosmetic industry as a surfactant, emulsifying agent and viscosity-inducing agent in emulsions or creams. Based on its chemical composition, Compritol 888 ATO is a blend of different esters of behenic acid with glycerol.Areas covered: Recently, there has been great interest in the multiple roles that Compritol 888 ATO plays in various pharmaceutical delivery systems. Accordingly, this review aimed at summarizing the current and potential applications of Compritol 888 ATO in various drug delivery areas.Expert opinion: Different researches have highlighted the feasibility of using Compritol 888 ATO as a lubricant or coating agent for oral solid dosage formulations. It has also been explored as a matrix-forming agent for controlling drug release. At present, the most common pharmaceutical application of Compritol 888 ATO is in lipid-based colloidal drug delivery system such as solid lipid microparticles, solid lipid nanoparticles...

Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake

Abstract: Docetaxel is a potent anticancer drug, but development of an oral formulation has been hindered mainly due to its poor oral bioavailability. In this study, solid lipid nanoparticles (SLNs) surface-modified by Tween 80 or D-alpha-tocopheryl poly(ethylene glycol 1000) succinate (TPGS 1000) were prepared and evaluated in terms of their feasibility as oral delivery systems for docetaxel. Tween 80-emulsified and TPGS 1000-emulsified tristearin-based lipidic nanoparticles were prepared by a solvent-diffusion method, and their particle size distribution, zeta potential, drug loading, and particle morphology were characterized. An in vitro release study showed a sustained-release profile of docetaxel from the SLNs compared with an intravenous docetaxel formulation (Taxotere®). Tween 80-emulsified SLNs showed enhanced intestinal absorption, lymphatic uptake, and relative oral bioavailability of docetaxel compared with Taxotere in rats. These results may be attributable to the absorption-enhancing effects of the tristearin nanoparticle. Moreover, compared with Tween 80-emulsified SLNs, the intestinal absorption and relative oral bioavailability of docetaxel in rats were further improved in TPGS 1000-emulsified SLNs, probably due to better inhibition of drug efflux by TPGS 1000, along with intestinal lymphatic uptake. Taken together, it is worth noting that these surface-modified SLNs may serve as efficient oral delivery systems for docetaxel.

Optimisation and stability assessment of solid lipid nanoparticles using particle size and zeta potential

Abstract: Solid lipid nanoparticles (SLNs) are a well-tolerated lipid carrier system due to the employment of a physiological and/or biodegradable lipid matrix. Physicochemical properties such as particle size, polydispersity index (PI) and zeta potential are SLN quality response parameters. Increased particle size is a good indicator of in-vitro instability. This work focuses on the importance of selecting the lipid matrices and excipients that can achieve the particle size and stability required if such formulations are to be utilised in the pharmaceutical market. With the aim of understanding the influence of variation in SLN composition (lipid and emulsifier concentration), a Taguchi model of experimental design was applied. Tested factors included the concentration of lipid (stearic acid) and the concentration of Tween20. SLNs were successfully prepared by a microemulsion-based technique. Based on the hydrophilic lipophilic balance (HLB), different combinations of emulsifiers/co-emulsifiers (Tween20/Span20, Tween20/Span80, Tween20/n-butanol, and Tween20/iso-propanol) were also used to control the physicochemical properties of SLNs. The influence of pH (addition of HCl or NaOH) and electrolyte (addition of NaCl), both during and after the preparation, were also investigated on selected SLN formulations. Slightly polydispersed (PI < 0.3) nanoparticles with a particle size < 450 nm and zeta potential range of +5 to –50 mV were developed. Physical stability of optimised stearic-acid based SLNs over 2 months were assessed by particle size measurement. SLNs were stable when refrigerated. These results suggest that thoughtful selection of lipid and lipid excipients is essential for successful preparation and physical stability of SLNs. This study facilitates the preliminary physicochemical characterisation for favourable encapsulation of lipophilic and hydrophilic drugs.

Topical delivery of ocular therapeutics: carrier systems and physical methods.

Abstract: Objective The basic concepts, major mechanisms, technological developments and advantages of the topical application of lipid-based systems (microemulsions, nanoemulsions, liposomes and solid lipid nanoparticles), polymeric systems (hydrogels, contact lenses, polymeric nanoparticles and dendrimers) and physical methods (iontophoresis and sonophoresis) will be reviewed. Key findings Although very convenient for patients, topical administration of conventional drug formulations for the treatment of eye diseases requires high drug doses, frequent administration and rarely provides high drug bioavailability. Thus, strategies to improve the efficacy of topical treatments have been extensively investigated. In general, the majority of the successful delivery systems are present on the ocular surface over an extended period of time, and these systems typically improve drug bioavailability in the anterior chamber whereas the physical methods facilitate drug penetration over a very short period of time through ocular barriers, such as the cornea and sclera. Summary Although in the early stages, the combination of these delivery systems with physical methods would appear to be a promising tool to decrease the dose and frequency of administration; thereby, patient compliance and treatment efficacy will be improved.

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies

Abstract: Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6–98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C 2°C and % relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration () and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).

Solid lipid nanoparticles-loaded topical gel containing combination drugs: an approach to offset psoriasis

Abstract: Aim: The primary aim of present work was to develop effective combination drug therapy for topical treatment of psoriasis.Methods: Betamethasone dipropionate and calcipotriol loaded solid lipid nanoparticles (CT-BD-SLNs) were prepared by hot melt high shear homogenization technique, which were then incorporated in Carbopol gel matrix. The anti-psoriatic potential was tested by sequential in vitro (skin permeation and dermal distribution, anti-proliferative effect in HaCaT cells) and in vivo (Draize patch irritation, transepidermal water loss (TEWL) and anti-psoriatic mouse tail studies) experiments.Results: A negligible amount in receptor compartment, yet confined distribution of drugs to epidermal and dermal region of skin was observed in case of SLNs, which is essential for safe and effective anti-psoriatic therapy. Draize patch test and TEWL demonstrated negligible skin irritation and better skin tolerability of SLNs. The in vitro HaCaT cell line study demonstrated that SLNs delayed the abrupt growth o...