β-cyclodextrin modification by cross-linking polymerization as highly porous nanomatrices for olanzapine solubility improvement; synthesis, characterization and bio-compatibility evaluation
TL;DR: In this paper, the authors reported highly porous and amorphous nanomatrices developed by cross-linking polymerization with subsequent condensation technique for solubility, dissolution and ultimately bioavailability enhancement of poorly soluble drug olanzapine (OLN).
About: This article is published in Journal of Drug Delivery Science and Technology.The article was published on 2021-11-08 and is currently open access. It has received 16 citations till now. The article focuses on the topics: Solubility & Dissolution.
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TL;DR: This is the first review presenting the contribution of natural polymers in the fabrication of eight polymeric NMs including particulate nanodelivery and nanofabrics with antibacterial and antibiofilm prospects, referring to modified polymer derivatives to explore their full potential for obtaining sustainable DD products.
Abstract: Despite the recent advancements in treating bacterial infections, antibiotic resistance (AR) is still an emerging issue. However, polymeric nanocarriers have offered unconventional solutions owing to their capability of exposing more functional groups, high encapsulation efficiency (EE) and having sustained delivery. Natural polymeric nanomaterials (NMs) are contemplated one of the most powerful strategies in drug delivery (DD) in terms of their safety, biodegradability with almost no side effects. Every nanostructure is tailored to enhance the system functionality. For example, cost-effective copper NPs could be generated in situ in cellulose sheets, demonstrating powerful antibacterial prospects for food safety sector. Dendrimers also have the capacity for peptide encapsulation, protecting them from proteolytic digestion for prolonged half life span. On the other hand, the demerits of naturally sourced polymers still stand against their capacities in DD. Hence, Post-synthetic modification of natural polymers could play a provital role in yielding new hybrids while retaining their biodegradability, which could be suitable for building novel super structures for DD platforms. This is the first review presenting the contribution of natural polymers in the fabrication of eight polymeric NMs including particulate nanodelivery and nanofabrics with antibacterial and antibiofilm prospects, referring to modified polymer derivatives to explore their full potential for obtaining sustainable DD products.
14 citations
TL;DR: In this article , a robust, highly stretchable self-healing elastomer with dynamic reversible multi-networks based on polyurethane matrix and cyclodextrin assembled nanosheets is proposed.
Abstract: Artificial materials with biomimic self‐healing ability are fascinating, however, the balance between mechanical properties and self‐healing performance is always a challenge. Here, a robust, highly stretchable self‐healing elastomer with dynamic reversible multi‐networks based on polyurethane matrix and cyclodextrin‐assembled nanosheets is proposed. The introduction of cyclodextrin nano‐assemblies with abundant surface hydroxyl groups not only forms multiple interfacial hydrogen bonding but also enables a strain‐induced reversible crystalline physical network owing to the special nanoconfined effect. The formation and dissociation of a dynamic crystalline physical network under stretching–releasing cycles skillfully balance the contradiction between mechanical robustness and self‐healing ability. The resulting nanocomposites exhibit ultra‐robust tensile strength (40.5 MPa), super toughness (274.7 MJ m−3), high stretchability (1696%), and desired healing efficiency (95.5%), which can lift a weight ≈ 100 000 times their own weight. This study provides a new approach to the development of mechanically robust self‐healing materials for engineering applications such as artificial muscles and healable robots.
6 citations
TL;DR: In this paper , a nano-version of hydrogels with the additional qualities of both hydrogel and nano-systems was synthesized to enhance the solubility and release characteristics of docetaxel by synthesizing highly porous and stimuli responsive nanosponges.
Abstract: This study aimed to enhance the solubility and release characteristics of docetaxel by synthesizing highly porous and stimuli responsive nanosponges, a nano-version of hydrogels with the additional qualities of both hydrogels and nano-systems. Nanosponges were prepared by the free radical polymerization technique and characterized by their solubilization efficiency, swelling studies, sol-gel studies, percentage entrapment efficiency, drug loading, FTIR, PXRD, TGA, DSC, SEM, zeta sizer and in vitro dissolution studies. In vivo toxicity study was conducted to assess the safety of the oral administration of prepared nanosponges. FTIR, TGA and DSC studies confirmed the successful grafting of components into the stable nano-polymeric network. A porous and sponge-like structure was visualized through SEM images. The particle size of the optimized formulation was observed in the range of 195 ± 3 nm. The fabricated nanosponges noticeably enhanced the drug loading and solubilization efficiency of docetaxel in aqueous media. The drug release of fabricated nanosponges was significantly higher at pH 6.8 as compared to pH 1.2 and 4.5. An acute oral toxicity study endorsed the safety of the system. Due to an efficient preparation technique, as well as its enhanced solubility, excellent physicochemical properties, improved dissolution and non-toxic nature, nanosponges could be an efficient and a promising approach for the oral delivery of poorly soluble drugs.
6 citations
TL;DR: In this article , pH-sensitive hydrogels were prepared via a free radical polymerization technique for the targeted delivery of 5aminosalicylic acid to the colon by cross-linked chitosan, β-Cyclodextrin, and acrylic acid.
Abstract: In the current research work, pH-sensitive hydrogels were prepared via a free radical polymerization technique for the targeted delivery of 5-aminosalicylic acid to the colon. Various proportions of chitosan, β-Cyclodextrin, and acrylic acid were cross-linked by ethylene glycol dimethacrylate. Ammonium persulfate was employed as an initiator. The development of a new polymeric network and the successful encapsulation of the drug were confirmed by Fourier transform infrared spectroscopy. Thermogravimetric analysis indicated high thermal stability of the hydrogel compared to pure chitosan and β-Cyclodextrin. A rough and hard surface was revealed by scanning electron microscopy. Similarly, the crystallinity of the chitosan, β-Cyclodextrin, and fabricated hydrogel was evaluated using powder X-ray diffraction. The swelling and drug release studies were performed in both acidic and basic medium (pH 1.2 and 7.4, respectively) at 37 °C. High swelling and drug release was observed at pH 7.4 as compared to pH 1.2. The increased incorporation of chitosan, β-Cyclodextrin, and acrylic acid led to an increase in porosity, swelling, loading, drug release, and gel fraction of the hydrogel, whereas a decrease in sol fraction was observed. Thus, we can conclude from the results that a developed pH-sensitive network of hydrogel could be employed as a promising carrier for targeted drug delivery systems.
5 citations
TL;DR: The developed PVP-K30-co-poly (AMPS) nanogel delivery system is expected to be safe, effective, and cost-effective for solubility improvement of poorly soluble drugs.
Abstract: Poor solubility is a global issue of copious pharmaceutical industries as large number of drugs in development stage as well as already marketed products are poorly soluble which results in low dissolution and ultimately dosage increase. Current study is aimed at developing a polyvinylpyrrolidone- (PVP-K30-) based nanogel delivery system for solubility enhancement of poorly soluble drug olanzapine (OLP), as solubilization enhancement is the most noteworthy application of nanosystems. Crosslinking polymerization with subsequent condensation technique was used for the synthesis of nanogels, a highly responsive polymeric networks in drug's solubility. Developed nanogels were characterized by percent entrapment efficiency, sol-gel, percent swelling, percent drug loaded content (%DLC), percent porosity, stability, solubility, in vitro dissolution studies, FTIR, XRD, and SEM analysis. Furthermore, cytotoxicity study was conducted on rabbits to check the biocompatibility of the system. Particle size of nanogels was found with 178.99 ± 15.32 nm, and in vitro dissolution study exhibited that drug release properties were considerably enhanced as compared to the marketed formulation OLANZIA. The solubility studies indicated that solubility of OLP was noticeably improved up to 36.7-fold in phosphate buffer of pH 6.8. In vivo cytotoxicity study indicated that prepared PVP-K30-based formulation was biocompatible. On the basis of results obtained, the developed PVP-K30-co-poly (AMPS) nanogel delivery system is expected to be safe, effective, and cost-effective for solubility improvement of poorly soluble drugs.
4 citations
References
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01 Jan 1965
TL;DR: Starch: Chemistry and Technology, Second Edition as discussed by the authors focuses on the chemistry, processes, methodologies, applications, and technologies involved in the processing of starch, including the history and future expectation of starch use, economics and future of the starch industry, and the genetics and physiology of starch development.
Abstract: Starch: Chemistry and Technology, Second Edition focuses on the chemistry, processes, methodologies, applications, and technologies involved in the processing of starch. The selection first elaborates on the history and future expectation of starch use, economics and future of the starch industry, and the genetics and physiology of starch development. Discussions focus on polysaccharide biosynthesis, nonmutant starch granule polysaccharide composition, cellular developmental gradients, projected future volumes of corn likely to be used by the wet-milling industry, and organization of the corn wet-milling industry. The manuscript also tackles enzymes in the hydrolysis and synthesis of starch, starch oligosaccharides, and molecular structure of starch. The publication examines the organization of starch granules, fractionation of starch, and gelatinization of starch and mechanical properties of starch pastes. Topics include methods for determining starch gelatinization, solution properties of amylopectin, conformation of amylose in dilute solution, and biological and biochemical facets of starch granule structure. The text also takes a look at photomicrographs of starches, industrial microscopy of starches, and starch and dextrins in prepared adhesives. The selection is a vital reference for researchers interested in the processing of starch.
2,002 citations
TL;DR: Amorphous pharmaceuticals are markedly more soluble than their crystalline counterparts, however, their experimental solubility advantage is typically less than that predicted from simplethermodynamic considerations.
Abstract: Purpose To evaluate the magnitude of the solubility advantage foramorphous pharmaceutical materials when compared to their crystallinecounterpartsMethods The thermal properties of several drugs in their amorphousand crystalline states were determined using differential scanningcalorimetry From these properties the solubility advantage for theamorphous form was predicted as a function of temperature using a simplethermodynamic analysis These predictions were compared to theresults of experimental measurements of the aqueous solubilities of theamorphous and crystalline forms of the drugs at several temperaturesResults By treating each amorphous drug as either an equilibriumsupercooled liquid or a pseudo-equilibrium glass, the solubilityadvantage compared to the most stable crystalline form was predicted to bebetween 10 and 1600 fold The measured solubility advantage wasusually considerably less than this, and for one compound studied indetail its temperature dependence was also less than predicted It wascalculated that even for partially amorphous materials the apparentsolubility enhancement (theoretical or measured) is likely to influencein-vitro and in-vivo dissolution behaviorConclusions Amorphous pharmaceuticals are markedly more solublethan their crystalline counterparts, however, their experimental solubility advantage is typically less than that predicted from simplethermodynamic considerations This appears to be the result of difficulties indetermining the solubility of amorphous materials under trueequilibrium conditions Simple thermodynamic predictions can provide a useful indication of the theoretical maximum solubility advantage foramorphous pharmaceuticals, which directly reflects the driving forcefor their initial dissolution
1,322 citations
TL;DR: In the pharmaceutical industry cyclodextrins have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs, and to increase their bioavailability and stability.
Abstract: Cyclodextrins are a family of cyclic oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity. Cyclodextrin molecules are relatively large with a number of hydrogen donors and acceptors and, thus, in general they do not permeate lipophilic membranes. In the pharmaceutical industry cyclodextrins have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs, and to increase their bioavailability and stability. Studies in both humans and animals have shown that cyclodextrins can be used to improve drug delivery from almost any type of drug formulation. However, the addition of cyclodextrins to existing formulations without further optimisation will seldom result in acceptable outcome. Currently there are approximately 30 different pharmaceutical products worldwide containing drug/cyclodextrin complexes on the market.
719 citations
TL;DR: Various mechanisms and reports relating to solubility enhancement using dendrimers, including ionic interaction, hydrogen bonding, and hydrophobic interactions are the possible mechanisms by which a d endrimer exerts its solubilizing property.
355 citations
TL;DR: The utility of cyclodextrin-based carriers like liposomes, niosomes, nanoparticles, micelles, millirods, and siRNA for delivery of antineoplastic agents, and various approaches used for the delivery are assessed.
Abstract: Most of the cytotoxic chemotherapeutic agents have poor aqueous solubility. These molecules are associated with poor physicochemical and biopharmaceutical properties, which makes the formulation difficult. An important approach in this regard is the use of combination of cyclodextrin and nanotechnology in delivery system. This paper provides an overview of limitations associated with anticancer drugs, their complexation with cyclodextrins, loading/encapsulating the complexed drugs into carriers, and various approaches used for the delivery. The present review article aims to assess the utility of cyclodextrin-based carriers like liposomes, niosomes, nanoparticles, micelles, millirods, and siRNA for delivery of antineoplastic agents. These systems based on cyclodextrin complexation and nanotechnology will camouflage the undesirable properties of drug and lead to synergistic or additive effect. Cyclodextrin-based nanotechnology seems to provide better therapeutic effect and sustain long life of healthy and recovered cells. Still, considerable study on delivery system and administration routes of cyclodextrin-based carriers is necessary with respect to their pharmacokinetics and toxicology to substantiate their safety and efficiency. In future, it would be possible to resolve the conventional and current issues associated with the development and commercialization of antineoplastic agents.
330 citations