Preparation and In Vitro-In Vivo Evaluation of Luteolin Loaded Gastroretentive Microsponge for the Eradication of Helicobacter pylori Infections

The current study aimed to develop a luteolin gastric floating microsponge for targeting Helicobacter pylori. The microsponge formulations were prepared by a quasi-emulsion method, and then evaluated for various physicochemical variables. The best microsponge was further assessed for drug-polymer interactions, surface morphology, in vivo floating, and in vitro anti H. pylori activity. The formulation which exhibited comparatively good production yield (64.45% ± 0.83), high entrapment efficiency (67.33% ± 3.79), prolonged in vitro floating time (>8 h), and sustained in-vitro drug release was selected as the best microsponge. The SEM study revealed that the best microsponge was spherical in shape and has a porous surface with interconnecting channels. DSC and XRD studies demonstrated the dispersion of luteolin in the polymeric matrix of the microsponge. Ultrasonography confirmed that the best microsponge could in the rat stomach for 4 h. The in vitro MIC results indicate that the anti H. pylori activity of the best microsponge was almost doubled and more sustained compared to pure luteolin. To conclude, it can be said that the developed luteolin gastric floating microsponge could be a better option to effectively eradicate H. pylori infections and the histopathological and pharmacodynamic assessments of our best microsponge can be expected to provide a rewarding outcome.

Intratracheally Inhalable Nifedipine-Loaded Chitosan-PLGA Nanocomposites as a Promising Nanoplatform for Lung Targeting: Snowballed Protection via Regulation of TGF-β/β-Catenin Pathway in Bleomycin-Induced Pulmonary Fibrosis

Pulmonary fibrosis is a serious ailment that may progress to lung remodeling and demolition, where the key participants in its incidence are fibroblasts responding to growth factors and cellular calcium swinging. Calcium channel blockers, like nifedipine (NFD), may represent auspicious agents in pulmonary fibrosis treatment. Unfortunately, NFD bears complicated pharmacodynamics and a diminished systemic bioavailability. Thus, the current study aimed to develop a novel, non-invasive nanoplatform for NFD for direct/effective pulmonary targeting via intratracheal instillation. A modified solvent emulsification–evaporation method was adopted for the fabrication of NFD-nanocomposites, integrating poly(D,L-lactide-co-glycolide) (PLGA), chitosan (CTS), and polyvinyl alcohol, and optimized for different physiochemical properties according to the 32 full factorial design. Additionally, the aerodynamic behavior of the nanocomposites was scrutinized through cascade impaction. Moreover, the pharmacokinetic investigations were conducted in rats. Furthermore, the optimum formulation was tested in bleomycin-induced pulmonary fibrosis in rats, wherein fibrotic and oxidative stress parameters were measured. The optimum nanocomposites disclosed a nanosized spherical morphology (226.46 nm), a high entrapment efficiency (61.81%) and a sustained release profile over 24 h (50.4%). As well, it displayed a boosted in vitro lung deposition performance with a mass median aerodynamic diameter of 1.12 µm. Pharmacokinetic studies manifested snowballed bioavailability of the optimal nanocomposites by 3.68- and 2.36-fold compared to both the oral and intratracheal suspensions, respectively. The intratracheal nanocomposites revealed a significant reduction in lung fibrotic and oxidative stress markers notably analogous to normal control besides repairing abnormality in TGF-β/β-catenin pathway. Our results conferred a compelling proof-of-principle that NFD-CTS-PLGA nanocomposites can function as a promising nanoparadigm for pulmonary fibrosis management.

Formulation And Evaluation Of Floating Microspheres Of Cefdinir

Various approaches have been used to retain the dosage form in the stomach as a way ofincreasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; andsuperporous hydrogel systems. The aim of this study was to prepare and evaluate floatingmicrospheres of cefdinir for the prolongation of gastric residence time. Themicrospheres were prepared byCapillary Extrusion method.A full factorial design was applied to optimize the formulation. The optimum batch of microsphere exhibited smooth surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 12 hrs, high entrapment efficiency upto68%.Scanning electron microscopy confirmed the hollown structure with particle size in the order of190 μm. The studies revealed that increase in concentration of gum Karaya increased the drug release from the floating microspheres.

Development of lipid-based microsuspensions for improved ophthalmic delivery of gentamicin sulphate

Aim: Anterior eye segment disorders are treated with eye drops and ointments, which have low ocular bioavailability necessitating the need for improved alternatives. Lipid microsuspension of gentamicin sulphate was developed for the treatment of susceptible eye diseases. Materials & methods: Lipid microsuspensions encapsulating gentamicin sulphate were produced by hot homogenization and evaluated. Ex vivo permeation and ocular irritancy tests were also conducted. Results & conclusion: Stable microsuspensions with high entrapment efficiency and satisfactory osmolarities were obtained. Release studies achieved 49–88% in vitro release at 12 h with sustained permeability of gentamicin compared with conventional gentamicin eye drop (Evril®). No irritation was observed following Draize’s test. The microsuspensions have great potential as ocular delivery system of gentamicin sulphate.

Pharmacosomes: An approach to improve biopharmaceutical properties of drugs basic considerations in development

Vesicular drug delivery systems including niososmes, liposomes, pharmacosomes, transferosomes, electrosomes, ethosomes, etc have been widely accepted for controlled delivery of the drug. Amongst, all these drug delivery systems pharmacosomes are gaining more attention of the researchers due to several benefits such as high entrapment efficiency, improved biopharmaceutical properties, and pharmacokinetic performance, no leakage or loss of drug, stability, etc. Pharmacosomes are amphiphilic phospholipid complexes of drugs having active hydrogen that bind to phospholipids and self-assembled into vesicles in an aqueous medium. Both hydrophilic and lipophilic drugs have been formulated into pharmacosomes that caused improved solubility and permeability of drugs. Pharmacosomes are prepared by using various techniques such as hand shaking method, ether injection, solvent evaporation method, supercritical fluid approach, etc and are characterized for prodrug confirmation, surface morphology, crystal state measurement, in vitro drug release, and stability, etc. Despite wide research and highly encouraging results in the preclinical studies, translation of these nanomedicines from laboratory to market has been very limited. The main aim of this review is to describe comprehensively the potential of pharmacosomes as a vesicular drug delivery system focusing mainly on their conventional and advanced methods of preparation, different characterization techniques, and their applications in the delivery of different types of drugs with improved biopharmaceutical properties and pharmacokinetic performance.

Formulation and Optimization of Butenafine-Loaded Topical Nano Lipid Carrier-Based Gel: Characterization, Irritation Study, and Anti-Fungal Activity

The present study aims to prepare and optimize butenafine hydrochloride NLCs formulation using solid and liquid lipid. The optimized selected BF-NLCopt was further converted into Carbopol-based gel for topical application for the treatment of fungal infection. Box Behnken design was employed to optimize the nanostructure lipids carriers (NLCs) using the lipid content (A), Tween 80 (B), and homogenization cycle (C) as formulation factors at three levels. Their effects were observed on the particle size (Y1) and entrapment efficiency (Y2). The selected formulation was converted into gel and further assessed for gel characterization, drug release, anti-fungal study, irritation study, and stability study. The solid lipid (Compritol 888 ATO), liquid lipid (Labrasol), and surfactant (tween 80) were selected based on maximum solubility. The optimization result showed a particle size of 111 nm with high entrapment efficiency of 86.35% for BF-NLCopt. The optimized BF-NLCopt converted to gel (1% w/v, Carbopol 934) and showed ideal gel evaluation results (drug content 99.45 ± 2.11, pH 6.5 ± 0.2, viscosity 519 ± 1.43 CPs). The drug release study result depicted a prolonged drug release (65.09 ± 4.37%) with high drug permeation 641.37 ± 46.59 µg (32.07 ± 2.32%) than BF conventional gel. The low value of irritation score (0.17) exhibited negligible irritation on the skin after application. The anti-fungal result showed greater efficacy than the BF gel at both time points. The overall conclusion of the results revealed NLCs-based gel of BF as an ideal delivery system to treat the fungal infection.

Formulation and Invitro characterization of Flurbiprofen loaded Nanosponges

The aim of this analysis is to see how effective a Nanosponge-loaded topical gel is at distributing flurbiprofen through the skin. Flurbiprofen was entrapped in Nanosponge and formulated into a gel for this purpose. Flurbiprofen Nanosponges were developed by solvent evaporation using pluronic F68 and ethyl cellulose. The particle size and entrapment quality were discovered to be in the range of 200-410 nm and 90.94% to 98.68%, respectively. For gel formulation, Nanopsonges with high entrapment efficiency and the smallest particle size (F3) were chosen based on the characterization. Using Guar gum, Carbopol, and HPMC K4M, a total of 6 formulations were produced to determine the sustained drug release and were tested for physiochemical tests, producing positive results. According to the findings of the above in vitro drug release trials, formulations containing carbopol release more drug at the end of 11 hours than other formulations and follow a zero-order with case II transport mechanism.

Formulation, Development and Assessment of Novel Phyto-Elastosomes Loaded with Devil’s Claw Extract

Background: Management of arthritis requires frequent administration of medications at high doses that may lead to unwanted side effects and diminished patient adherence to the therapy. Devil’s claw extract, a herbal medicine from the Kalahari sands possess similar therapeutic efficacy with less side effects as the commercialized NSAIDs. The objectives of this study were to formulate, develop and assess novel phyto-elastosomes loaded with Devil’s claw extract in order to combat the toxicity levels associated with Devil’s claw and enhance penetration of harpagoside to intended targeted site.Methods: Screening studies were undertaken to determine the ideal amount of Tween® 80, cholesterol, ethanol, diacetyl phosphate and the pH of the hydration medium necessary to produce stable Devil’s claw-loaded phyto-elastosomes. Parameters monitored were particle size, polydispersity index, zeta potential, entrapment efficiency and deformability index.Results: The use of 20 % v/v ethanol was sufficient to produce novel phyto-elastosomes capable of deforming with minimal size alterations. Hydration of thin films in acidic solution produced phyto-elastosomal dispersions with high entrapment efficiency. The presence of cholesterol impeded harpagoside entrapment and increased cholesterol content affected the stability of vesicles by causing agglomeration. Conversely, increasing Tween® 80 concentration promoted harpagoside entrapment. Diacetyl phosphate promoted the stability of vesicle through charge induction.Conclusions: Development of Devil’s claw loaded phyto-elastosomes is useful in ensuring harpagoside reach the target site of action in arthritis-affected patients. Incorporation of these elastic vesicles in transdermal dosage forms may significantly improve the management of arthritis in the near future.

Nanotechnology Based Cosmeceuticals

Nanotechnology manifests the progression within stage of research and development, by increasing the efficacy of the merchandise through delivery of innovative solutions. to beat certain drawbacks associated with the traditional products, application of nanotechnology is escalating within the world of cosmeceuticals. In private care industry, cosmeceuticals are considered the fastest growing segment and thus the use has risen drastically over the years. Nanocosmeceuticals used for skin, hair, nail, and lip care, for conditions like wrinkles, photoaging, hyperpigmentation, dandruff, and hair damage, have inherit widespread use. Novel nanocarriers like nano emulsions, liposomes, microemulsions, niosomes, solid lipid nanoparticles, nanospheres and nanostructured lipid carrier have replaced the usage of conventional delivery system. These novel nanocarriers have advantages of controlled and sustained drug release, enhanced skin penetration, higher stability, high entrapment efficiency and site-specific targeting. However, nanotoxicological researches have indicated concern regarding the impact of increased use of nanoparticles in cosmeceuticals as there are possibilities of nanoparticles to penetrate through skin and cause health hazards. This review on nanotechnology utilized in cosmeceuticals highlights the various novel carriers used for the delivery of cosmeceuticals, marketed formulations, their positive and negative aspects, toxicity, and regulations of nanocosmeceuticals.

Preparation and Characterization of Liposomal Everolimus by Thin-Film Hydration Technique

In 10% to 40% of the cases of coronary stent implantation, patients face in-stent restenosis due to an inflammatory response, which induces artery thickening. Everolimus, a drug that inhibits growth factor-stimulated cell proliferation of endothelial cells, represents a promising alternative to prevent in-stent restenosis. In this study, everolimus was encapsulated by a film hydration technique in liposomes by using phosphatidylcholine and cholesterol at different ratios. As the ratio of cholesterol increases, it modulates the rigidity of the structure which can affect the encapsulation efficiency of the drug due to steric hindrance. Moreover, various lipid : drug ratios were tested, and it was found that as the lipid : drug ratio increases, the encapsulation efficiency also increases. This behavior is observed because everolimus is a hydrophobic drug; therefore, if the lipidic region increases, more drug can be entrapped into the liposomes. In addition, stability of the encapsulated drug was tested for 4 weeks at 4°C. Our results demonstrate that it is possible to prepare liposomal everolimus by film hydration technique followed by extrusion with high entrapment efficiency as a viable drug delivery system.