Riyaz Ali M. Osmani

Microsponges based novel drug delivery system for augmented arthritis therapy

The motive behind present work was to formulate and evaluate gel containing microsponges of diclofenac diethylamine to provide prolonged release for proficient arthritis therapy. Quasi-emulsion solvent diffusion method was implied using Eudragit RS-100 and microsponges with varied drug–polymer ratios were prepared. For the sake of optimization, diverse factors affecting microparticles physical properties were too investigated. Microsponges were characterized by SEM, DSC, FT-IR, XRPD and particle size analysis, and evaluated for morphology, drug loading, in vitro drug release and ex vivo diffusion as well. There were no chemical interactions between drug and polymers used as revealed by compatibility studies outcomes. The drug polymer ratio reflected notable effect on drug content, encapsulation efficiency and particle size. SEM results revealed spherical microsponges with porous surface, and had 7.21 μm mean particle size. The microsponges were then incorporated in gel; which exhibited viscous modulus along with pseudoplastic behavior. In vitro drug release results depicted that microsponges with 1:2 drug–polymer ratio were more efficient to give extended drug release of 75.88% at the end of 8 h; while conventional formulation get exhausted incredibly earlier by releasing 81.11% drug at the end of 4 h only. Thus the formulated microsponge-based gel of diclofenac diethylamine would be a promising alternative to conventional therapy for safer and efficient treatment of arthritis and musculoskeletal disorders.

Intra-articular delivery of a methotrexate loaded nanostructured lipid carrier based smart gel for effective treatment of rheumatic diseases

A nanostructured lipid carrier (NLC) based smart gel of methotrexate (MTX) was developed as a potential system for the treatment of rheumatic diseases (RD). NLC composed of Compritol ATO 888 as the solid lipid, Capmul MCM EP as the liquid lipid, Tween 80 as the surfactant and PEG 400 as the co-surfactant was prepared by modified hot homogenization followed by melt ultrasonication. The prepared NLC dispersion was characterized for particle size, polydispersity index (PDI), entrapment efficiency and zeta potential. The nanoparticulate dispersion was suitably gelled into the polymer matrices of Pluronic F-127 (PF-127) and Pluronic F-68 (PF-68). Two-factor three-level full factorial design was employed to determine the optimum concentrations of PF-127 and PF-68. The prepared NLC based smart gel was evaluated for viscosity, sterility, thermosensitivity, syringeability, content uniformity and in vitro release behaviour. The efficacy and biocompatibility of the NLC based smart gels were established using an adjuvant arthritis model and histology analysis, respectively. The NLCs had an average particle size of 107 ± 6 nm with a PDI of 0.365 ± 0.03, entrapment efficiency of 69.53% ± 1.23% and zeta potential of −13.54 ± 1.1 mV. The optimized NLC based smart gel (F-10) was found to be thermo-sensitive and exhibited 92.41% drug release at 108 h. The results demonstrated that MTX was evenly distributed in the optimized formulation, which was sterile and syringeable through an 18 gauze needle. A significant decrease in rat joint swelling was observed using the MTX-NLC based gel during a 28 day period. In conclusion, this MTX-NLC based gel could be a potential formulation for intra-articular treatment of inflammation in rheumatic conditions.

Polyacrylamide grafted guar gum based glimepiride loaded pH sensitive pellets for colon specific drug delivery: fabrication and characterization

Purpose: The purpose of this study was to prepare pH-sensitive pellets using an extrusion-spheronization pelletization (ESP) technique. Method: Polyacrylamide-grafted-guar gum (pAAm-g-GG) was prepared by taking three different ratios of guar gum to acrylamide (1 : 2, 1 : 3.5 and 1 : 5). Amide groups of these grafted copolymers were converted into carboxylic functional groups. Fourier transform infrared (FT-IR) spectroscopy, Differential Scanning Calorimetry (DSC) and 1H-NMR spectroscopy were used to characterize the grafted copolymers. Pellets were prepared by pAAm-g-GG (1.0–4.5%) and microcrystalline cellulose incorporating an anti-diabetic drug viz., glimepiride. Here, variables were studied and pellets were characterized for average size, surface morphology, friability, bulk density and flow properties. In vitro drug release was carried out in simulated gastric and intestinal conditions. Result: The in vitro drug release profile indicated an increase in drug release retardation with increasing pAAm-g-GG concentration. The formulated pellets were stable with respect to their physicochemical characters and drug content over a period of 60 days at different temperatures and relative humidity. Conclusion: It has been concluded that the prepared pellets demonstrate the potential use of MCC and pAAm-g-GG for the development of pH sensitive colon specific controlled drug delivery systems of glimepiride for diabetic therapy.

Recent Advances in Nanosystems and Strategies for Managing Leishmaniasis.

BACKGROUND Parasitic infection such as leishmaniasis, a neglected tropical disease, presents a significant global burden which is responsible for high mortality rate especially in less developed countries. Its intracellular nature and disseminated locations of parasite, limited number of chemotherapeutic agents, increasing incidences of resistance to first line drugs and toxicities, pose a great challenge to formulation scientists that have necessitated effective management of leishmanial infection by modulating the delivery of existing drugs. Over the past decade, research on development of alternative treatments such as nanotechnology-based drug delivery systems (nanoparticles, nanosuspensions, liposomes etc.), use of natural products as well as development of antileishmanial vaccine has been extensively investigated. OBJECTIVE The present review focuses on different facets of therapeutic strategies, existing miscellaneous drug delivery systems and approaches intended for management, as well as treatment of the infection, with an objective to summarize the current trends and strategies adopted for antileishmanial therapy in a systematic manner. Moreover, the article encloses an eclectic collection of patents allied to new-fangled chemotherapeutics for antileishmanial therapy. CONCLUSION The reported miscellaneous novel drug delivery systems along with the diverse approaches are seem to be precise, secure and relatively effective; and in an outcome, could lead to the new track for management of leishmaniasis.

A 32 full factorial design for development and characterization of a nanosponge-based intravaginal in situ gelling system for vulvovaginal candidiasis

Clotrimazole (CTZ) is a Biopharmaceutics Classification System (BCS) Class II drug having a limited therapeutic potential because of its poor aqueous solubility and relatively short half-life. The rationale behind the present research effort was to enhance the solubility and efficacy of CTZ by having it form a complex with hydroxypropyl β-cyclodextrin (HP-β-CD) nanosponges. Nanosponges (NSs) are hyper-cross linked cyclodextrin polymer-based colloidal structures with three-dimensional networks. Herein, NSs were prepared using dimethyl carbonate as a cross linker, suitably gelled, and were assessed for in vitro release, in vitro bioadhesion, in vivo antifungal activity and in vivo irritation using female Wistar albino rats. Nine formulations were prepared based on a 32 full factorial design using different Pluronic F-127: Pluronic F-68 ratios. The prepared CTZ-HP-β-CD NS samples were characterized by carrying out SEM, TEM, and FT-IR spectroscopy studies, as well as DSC and XRPD studies. The average particle size of loaded NS (N6) was found to be 455.6 nm. This sample displayed the lowest polydispersity index of the samples tested, and displayed a high zeta potential (−21.32 ± 1.3 mV), indicative of a stable colloidal nanosuspension. The optimized CTZ NS-based in situ gel (F-10) demonstrated prolonged drug release (up to 15 h), considerably longer than that of the conventional in situ gel, whose drug release only lasted for less than 6 h. The CTZ-NS gel showed higher in vivo antifungal activity and in vitro bioadhesion than did the conventional in situ gel. Furthermore, in vivo irritation studies showed the optimized CTZ NS gel formulation to be a non-irritant. All of these results signified the promising applicability of the formulated CTZ NS gel as a novel delivery system for the local treatment of vaginal candidiasis and other similar infections.

Fabrication, characterization, and evaluation of microsponge delivery system for facilitated fungal therapy

Objective: The rationale behind present research vocation was to develop and investigate a novel microsponge based gel as a topical carrier for the prolonged release and cutaneous drug deposition of fluconazole (FLZ); destined for facilitated fungal therapy. Materials and Methods: Microsponges were prepared using quasi-emulsion solvent diffusion method using Eudragit S-100. In the direction of optimization, the effect of formulation variables (drug-polymer ratio and amount of emulsifier) and diverse factors affecting physical characteristics of microsponge were investigated as well. Fabricated microsponges were characterized by differential scanning calorimetry, Fourier transform-infrared, scanning electron microscopy (SEM), particle size analysis, and also evaluated for drug content, encapsulation efficiency, in vitro drug release and in vitro antifungal activity. Results: Compatibility studies results reflected no sign of any chemical interaction between the drug and polymers used. Whereas, varied drug-polymer ratios and emulsifier concentration indicated significant effect on production yield, drug content, encapsulation efficiency, particle size and drug release. Spherical microsponges with a porous surface and 29.327 ± 0.31 μm mean particle size were evident from SEM micrographs. In vitro release outcomes, from microsponge loaded gels depicted that F1 formulation was more efficient to give extended drug release of 85.38% at the end of 8 h, while conventional formulation by releasing 83.17% of drug got exhausted incredibly earlier at the end of 4 h merely. Moreover, microsponge gels demonstrated substantial spreadability and extrudability along with promising antifungal activity. Conclusions: Fabricated microsponges would be impending pharmaceutical topical carriers of FLZ and a leading alternative to conventional therapy for efficient, safe and facilitated eradication of fungal infections.

Nanosponge Carriers- An Archetype Swing in Cancer Therapy: A Comprehensive Review.

Nanotechnology and nanomedicines are emerging research meadows; which chiefly focuses on creating and manipulating materials at a nanometer level for the betterment in imaging, diagnosis and treatment of a range of diseases together with cancer. Cyclodextrin-based nanosponges, anticipated as a new-fangled nanosized delivery system, are ground-breaking hyper-crosslinked cyclodextrin polymers nanostructured within a three-dimensional network. Nanosponges based systems hold the potential of elevating the solubility, absorption, penetration, bioavailability, in vivo stability, targeted as well as sustained delivery, and therapeutic efficiency of numerous anticancer agents. The extension of nanosponges based drug delivery systems is an exhilarating and demanding research pasture, predominantly to overcome aforementioned problems allied to existing anticancer formulations and for the further progressions in cancer therapies. Nanosponges in cancer therapy, particularly cyclodextrin based nanosponges are brought up in this review. By quoting diverse attempts made in pertinent direction, efforts have been made to exemplify the characteristics, suitability and versatility of cyclodextrin based nanosponges for their promising applications in cancer treatment.

Current Perspectives on Novel Drug Delivery Systems and Approaches for Management of Cervical Cancer: A Comprehensive Review

Cervical cancer is uterine cervix carcinoma, the second deadly cancer and has a high incidence and mortality rate. In the developing world conventional treatment strategies such as surgical intervention and chemoradiotherapy are less widely available. Currently cancer research focuses on improving treatment of cervical cancer using various therapies such as gene therapy, recombinant protein therapy, photodynamic therapy, photothermal therapy and delivery of chemotherapeutic agents using nanoparticles, hydrogel and liposomal based delivery systems and also localized delivery systems which exist in a variety of forms such as intravaginal rings, intravaginal patches, intravaginal films, etc. in order to improve the drug delivery in a controlled manner to the diseased site thereby reducing systemic side effects. The present review encloses existing diverse delivery systems and approaches intended for treatment of cervical cancer.

Current Perspectives on Novel Drug Delivery Systems and Therapies for Management of Prostate Cancer: An Inclusive Review

BACKGROUND Prostate cancer (PC) is a prostate gland cells carcinoma, the foremost reason of cancer deaths in men in developed countries, representing most common malignancy in adult males. The key obstacle to achieve practicable therapeutic effect of active drugs and capable hopeful agents including proteins and peptides, and nucleic acid for prostate cancer is the scarcity of targeted drug delivery to cells of prostate cancer. As a result, need for novel systems, strategies or therapeutic approaches to enhance the assortment of active agents meant for prostate cancer becomes an important criterion. Currently cancer research focuses on improving treatment of prostate cancer using various novel drug delivery systems of chemotherapeutic agents. These novel drug delivery systems comprise nanoparticles and liposomes. Also, strategies or therapeutic approaches intended for the prostate cancer include radiation therapy for localized prostate cancer, hormonal therapy for suppressing tumor growth, and gene-and-immunologic therapy. These systems and approaches can deliver the drugs to their selected or targeted cancer cells for the drug release in cancer atmosphere of prostate thereby enhancing the effectiveness of tumor penetration. OBJECTIVE The objective was to collect and report the recent research findings to manage the PC. Present review encloses existing diverse novel drug delivery systems and approaches intended for the management of PC. CONCLUSION The reported miscellaneous novel drug delivery systems along with the diverse therapies are seem to be precise, secure and relatively effective; and in consequence could lead to a new track for obliteration of prostate cancer.

Fabrication and characterization of carboxymethylated bael fruit gum with potential mucoadhesive applications

A study was conducted to enhance the mucoadhesive potential of bael fruit gum by carboxymethylation. Carboxymethylation of bael fruit gum was achieved through its reaction with monochloroacetic acid in the presence of sodium hydroxide as a catalyst under different reaction conditions. The optimal degree of substituted carboxymethyl in the carboxymethylated bael fruit gum was found to be 0.68. The resulting product was characterized by FT-IR, DSC, XRD and SEM analyses. The results revealed that the carboxymethylated derivative of bael fruit gum showed an improved mucoadhesive potential compared to unmodified gum, with a slightly increased degree of crystallinity, surface roughness and decreased viscosity. Additionally, metformin-loaded, ionotropically gelled beads of bael fruit gum and carboxymethylated bael fruit gum were formulated using calcium chloride as a cross-linking agent. An ex vivo bioadhesion study performed by a wash-off test using goat intestinal mucosa showed higher bioadhesion times for carboxymethylated bael fruit gum compared to bael fruit gum. In vitro release studies conducted using phosphate buffer (pH 6.8) showed a faster release of metformin from carboxymethylated bael fruit gum than from bael fruit gum. These results have demonstrated that carboxymethylated bael fruit gum is a promising mucoadhesive excipient.