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Shah M.,Rajiv Academy for Pharmacy | Pathak K.,Rajiv Academy for Pharmacy
AAPS PharmSciTech | Year: 2010

The objective of this study was to develop solid lipid nanoparticles (SLNs) of simvastatin and to optimize it for independent variables (amount of glycerol monostearate, concentration of poloxamer, and volume of isopropyl alcohol) in order to achieve desired particle size with maximum percent entrapment efficiency (% EE) and percent cumulative drug release (% CDR). To achieve our goal, eight formulations (F1-F8) of SLNs were prepared by solvent injection technique and optimized by 23 full-factorial design. The design was validated by extra design checkpoint formulation (F 9), and the possible interactions between independent variables were studied. The responses of the design were analyzed using Design Expert 7.1.6. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw Pareto charts and response surface plots. On the basis of software analysis, formulation F10 with a desirability factor of 0.611 was selected as optimized formulation and was evaluated for the independent parameters. Optimized formulation showed particle size of 258.5 nm, % EE of 75.81%, with of 82.67% CDR after 55 h. The release kinetics of the optimized formulation best fitted the Higuchi model, and the recrystallization index of optimized formulation was found to be 65.51%. © 2010 American Association of Pharmaceutical Scientists.

Sharma G.K.,Rajiv Academy for Pharmacy | Pathak D.,Rajiv Academy for Pharmacy
Chemical and Pharmaceutical Bulletin | Year: 2010

Solvent free microwave assisted synthesis of some novel substituted imidazoles of biological interest is reported. First, primary aromatic or heteryl amine was condensed with aryl or heteryl aldehydes to afford corresponding Schiff's base. The Schiff's base further on treatment with ammonium acetate (NH 4OAC) and isatin using silica gel as the solid support, yielded the corresponding aryl imidazoles. In this paper a comparative study between the developed microwave method and conventional method is described. The synthesized compounds were analyzed by physical and analytical data. The synthesized compounds were evaluated for their antibacterial, anthelmintic, short-term anticancer and antitubercular activity. All the synthesized substituted imidazoles have shown good antibacterial activity against gram negative bacterial strains Klebsiella pneumoniae and Escherichia coli and moderate to good anthelmintic activity. The synthesized imidazole derivative possessed signifi-cant cytotoxic activity against Ehrlich's ascites carcinoma (EAC) cell lines. None of the compounds exhibited prominent antitubercular activity. © 2010 Pharmaceutical Society of Japan.

Pathak M.K.,Rajiv Academy for Pharmacy | Chhabra G.,Rajiv Academy for Pharmacy | Pathak K.,Rajiv Academy for Pharmacy
Drug Development and Industrial Pharmacy | Year: 2013

The objective of the present research was to develop a novel pH triggered nanoemulsified in-situ gel (NE-ISG) for ophthalmic delivery of fluconazole (FLZ) to enhance the permeation and residence time of the formulation, by overcoming the limitations associated with protective ocular barriers. Pseudoternary phase diagrams were constructed using capmul MCM (oil phase), tween 80 (surfactant) and transcutol P (cosurfactant) to identify the NE region. Nanoemulsions (NE1-NE6) of FLZ were prepared by spontaneous emulsification method and evaluated for various pharmacotechnical characteristics. NE4 was selected as optimized NE and was dispersed in carbopol 934 solution to form nanoemulsified sols (NE-ISG1 to NE-ISG5) that were expected to convert in to in-situ gels at corneal pH (7.4). The optimized NE-ISG was selected on the basis of gelation ability with a residence time up to or more than 6 h. Ex-vivo transcorneal permeation study displayed significantly higher (p<0.05) permeation of FLZ from NE-ISG5 (337.67 μg/cm2) and NE4 (419.30 μg/cm2) than the commercial eye drops (112.92 μg/cm2). Hen's egg test-Chorioallantoic membrane (HET-CAM) test with zero score indicated the non-irritant property of developed NE-ISG5. Corneal toxicity study revealed no visual signs of tissue damage. Hence it can be concluded that NE-ISG5 may offer a more intensive treatment of ocular fungal infections due to higher permeation, prolonged precorneal residence time and sustained drug release along with higher in-vitro efficacy, safety and greater patient compliance. © 2013 Informa Healthcare USA, Inc.

Sharma P.,Rajiv Academy for Pharmacy | Pathak K.,Rajiv Academy for Pharmacy
Expert Opinion on Biological Therapy | Year: 2012

Introduction: Rheumatoid arthritis (RA) is a chronic inflammatory joint disorder that is characterized by inflammation of synovial membrane and the release of inflammatory cytokines that ultimately results in joint destruction and disability. The therapeutic treatment plan for treating RA patient initiates with disease-modifying antirheumatic agents (DMARDs) and ends with the use of biological agents. Sometimes a combination of DMARDs and the biological agents are aggressively initiated. But this is not sufficient to retard the underlying progression of the disease and hence the disease-associated pain persists. The solution lies in the treatment of causative factors. Modern therapy aims at targeting newer target sites that can not only overcome the problem of pain and disability but also minimize the occurrence of adverse effects faced by the traditional therapeutic approach. Areas covered: This review covers the pathological background of the disease in brief, the traditional and newer biologicals, therapeutic targets and novel therapies for rheumatoid arthritis. Expert opinion: Better management of the disease can be achieved by focusing on the causes and the factors of the disease. Newer therapies and targeting sites discussed in this review focus on treating the disability at the cellular level without affecting body's immune response and minimizing the chances of infection and inflammation. © Informa UK, Ltd.

Pathak K.,Rajiv Academy for Pharmacy | Raghuvanshi S.,Rajiv Academy for Pharmacy
Clinical Pharmacokinetics | Year: 2015

The delivery of drugs through the oral route is regarded as most optimal to achieve desired therapeutic effects and patient compliance. However, poor pharmacokinetic profiles of oral drug candidates remains an area of concern, and approaches to enhance their bioavailability are widely cited in the literature. Traditionally, the approaches have been confined to molecular optimization of the drug molecule, which has gradually evolved into development of microsized and nanosized formulations. Nanoformulations, by virtue of their nanosize, are widely acclaimed for circumventing the obstacles of poor pharmacokinetics. In this review, an attempt has been made to discuss existing challenges of bioavailability and approaches to overcome the same, with in-depth compilation of the literature on nanoformulations. The nanoformulations reviewed include nanocrystals, nanoemulsions, polymeric nanoparticles, self-nanoemulsifying drug delivery systems, dendrimers, carbon nanotubes, polymeric micelles and lipid nanocarriers. This review confirms the potential of nanomedicines to improve the pharmacokinetics of drugs via nanoformulations. Chemotherapeutic applications and patent reports are also compiled in the review. Despite the promising benefits, nanomedicines are associated with hazards to human health. Hence, the review also deals with toxicological consequences of nanomedicines, and with in vitro/in vivo screening methods to assess bioavailability as per regulatory considerations. Nanotechnology has been shown to facilitate the clinical translation of drug candidates that were deemed to be bioavailability failures. Conclusively, nanotechnological approaches to particle design and formulation are beginning to expand the market for many drugs with improved bioavailability and therapeutics. However, dedicated efforts are needed to develop advanced nanomedicines with minimal or no adverse effects. © 2015, Springer International Publishing Switzerland.

Rajpoot P.,Rajiv Academy for Pharmacy | Pathak K.,Rajiv Academy for Pharmacy | Bali V.,Rajiv Academy for Pharmacy
Recent Patents on Drug Delivery and Formulation | Year: 2011

Nanoemulsions have garnered considerable attention in research as well as in therapeutics due to their advantages like thermodynamic stability, optical clarity, ease of preparation, and unique property of behaving as supersolvent for solubilizing both hydrophobic and hydrophilic solutes. Due to above mentioned attributes, nanoemulsions find numerous applications in diagnosis as well as therapy of diseases. Hence, the aim of the current review is to recapitulate these applications of this novel drug delivery system by discussing the patents governing various applications of this system. © 2011 Bentham Science Publishers Ltd.

Kumar A.,Rajiv Academy for Pharmacy | Pathak K.,Rajiv Academy for Pharmacy | Bali V.,Rajiv Academy for Pharmacy
Drug Discovery Today | Year: 2012

The skin acts as a barrier and prevents transcutaneous delivery of therapeutic agents. Transferosomes are novel vesicular systems that are several times more elastic than other vesicular systems. These are composed of phospholipids, edge activator and ethanol and are applied in a non-occlusive manner. Owing to their ultradeformability, they have the potential to deliver therapeutic agents across the intact skin in a non-invasive and non-allergenic manner. The present review attempts to provide an in-depth account of ultra-adaptable nanovesicular systems. The current investigation, besides compiling existing knowledge in a systematic manner, also includes information like regulatory aspects of excipients used in preparation, summary of clinical investigations performed, marketed preparations available, research reports and patent reports related to transfersomes. © 2012 Elsevier Ltd.

Pathak K.,Rajiv Academy for Pharmacy
Expert Opinion on Therapeutic Targets | Year: 2014

Introduction: The discovery of IL-7 and thymic stromal lymphopoietin (TSLP) has been a major step in the understanding of arthritis. IL-7 amplifies the inflammation induced by other cytokines, primarily TNF. In animal models of arthritis, inhibition of IL-7 limits inflammation and joint erosion. TSLP is an IL-7-like cytokine that triggers dendritic cell-mediated Th2-type inflammatory responses and is considered as a master switch for allergic inflammation. TSLP is a downstream molecule of TNF-α and as such may be involved in the pathophysiology of inflammatory arthritis. Areas covered: This review summarizes current knowledge of the role of IL-7 and TSLP derived from both animal models and studies in patients with rheumatoid arthritis (RA). The emergence of IL-7 blockade as a future therapy in RA is highlighted, along with the potential goals and limitations of this therapeutic approach. The write-up also highlights the functional capacities of TSLP in arthritis. Expert opinion: Evidences suggest important roles for IL-7 and TSLP in the pathogenesis of RA and can be viewed as potential therapeutic targets. Regulation of these at genetic level is a promising investigational area. Given the difficulty in reconstituting T cells in patients with RA, therapeutic approaches that minimize the elimination of T cells are likely to be more desirable. © 2014 Informa UK, Ltd.

Verma P.,Rajiv Academy for Pharmacy | Pathak K.,Rajiv Academy for Pharmacy
Nanomedicine: Nanotechnology, Biology, and Medicine | Year: 2012

This project aimed at developing nanovesicles of econazole nitrate (EN) and formulating them as a suitable dermatological gel for improved therapeutic efficacy, better dispersity, and good storage stability. Ethosomes were prepared by cold method and evaluated for the mean diameter, surface charge, and entrapment efficiency. Optimized ethosomes with vesicle size and entrapment efficiency of 202.85 ± 5.10 nm and 81.05 ± 0.13%, respectively, were formulated as Carbopol 934 NF gels with varied permeation enhancers (G1-G7), and compared with liposomal and hydroethanolic gels. The pharmacotechnical evaluation of gels demonstrated G6 with a flux rate of 0.46 ± 0.22 μg/cm 2 hr 1/2 as the best formulation that was able to exhibit controlled release of EN for 12 hours across rat skin, and percent drug diffused from ethosomes was nearly twofold higher than liposomal and hydroethanolic gels. Confocal laser scanning microscopy demonstrated drug permeation as far as the last layer of epidermis (stratum basale). Stability profile of the prepared system assessed for 180 days revealed very low aggregation and insignificant growth in vesicular size. The results collectively suggest that because of the controlled drug release, better antifungal activity, and good storage stability, EN ethosomal gel has tremendous potential to serve as a topical delivery system. From the Clinical Editor: Ethosomal gel of econazole nitrate was found to have outstanding potential to serve as a topical delivery system, enabling controlled drug release, providing better antifungal activity, and good storage stability. © 2012 Elsevier Inc.

The investigation was aimed at developing thermodynamically stable topical delivery system of nanostructured lipid carrier of econazole nitrate (EN) for the treatment of deep seated fungal infection by improving its permeability. Fifteen formulations (F1-F15) of nanostructured lipid carriers (NLCs) were prepared by solvent injection technique using central composite design and characterized for particle size and % entrapment efficiency. Closeness in the results, guided the selection of five NLC formulations which were formulated as hydrogels (G1-G5) using Carbopol 934. The permeation studies of gels demonstrated G3 with flux rate of 3.21 ± 0.03 μg/cm(2)/min (> target flux of 1.46 μg/cm(2)/min) as the best formulation that exhibited zero order permeation. The amount of drug/unit area demonstrated linear dependency on flux rate. Confocal laser scanning microscopy demonstrated penetration of rhodamine red till the stratum basale due to hydration of stratum corneum. Hydrogel G3 containing NLC formulation (F5) was selected as the optimized topical gel. TEM of F5 revealed spherical particles that presented low recrystallization index of 72.35%. Stability profile for 90 days revealed insignificant change (p < 0.05) in the particle size and zeta potential indicating substantial stability of the system. Thus, EN-loaded NLC indicated better permeability and thermodynamic stability as effective topical delivery system for deep seated fungal infection.

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