Himanshu Gupta

NCTR/FDA (Nat'l. Center for Toxicological Research), Pharmaceutics, Faculty Member

Jamia Hamdard, Department of Pharmaceutics, Alumnus

Organization of Pharmaceutical Unity with BioAllied Sciences, Educational Society, Gen Sec

University of Colorado Denver, Department of Pharmaceutical Sciences, Post-Doc

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Supervisors: Organization of Pharmaceutical Unity with Bioallied Sciences (OPUBS), Journal of Pharmacy & BioAllied Sciences, Recent patents in drug delivery & formulation, Chronicles of Young Scientists, and OPUBS

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Himanshu Gupta

Delhi Technological University, Delhi, India

Chitkara University

University of Mississippi

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Kamala Kumari V E N K A T A Paravastu

Mohammad Samim

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Papers by Himanshu Gupta

Nanoparticles ladenin situgel of levofloxacin for enhanced ocular retention

Drug Delivery, 2013

Availability of proper concentration of medicament on to the corneal surface is a challenging tas... more Availability of proper concentration of medicament on to the corneal surface is a challenging task. Many novel formulations, i.e. hydrogels, nanoparticles, ocuserts, etc. had been tested to improve ocular bioavailability, out of which our group found, in situ gel and polymeric nanoparticle are the most interesting approach to achieve ocular retention. We found that in situ gel stay only for 12 h and poly(lactic-co-glycolic acid (PLGA) nanoparticles are non mucoadhesive in nature so we try to combine both these formulations and termed it as ''Nanoparticle laden in situ gel''. Here we prepare nanoparticle laden in situ gel containing levofloxacin encapsulated PLGA nanoparticle, incorporated in chitosan in situ gel and evaluated its ocular retention by gamma scintigraphy in rabbits. The observations of acquired gamma camera images showed good retention over the entire precorneal area. From static and dynamic gamma scintigraphy evaluation, we can be interpret that developed nanoparticle laden in situ gel formulation cleared at a very slow rate and remained at corneal surface for longer duration than marketed formulation, in situ gel and nanosuspension alone.

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Nanoparticles ladenin situgel of levofloxacin for enhanced ocular retention

Drug Delivery, 2013

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Nanoparticle laden in situ gel for sustained ocular drug delivery

Journal of Pharmacy & BioAllied Sciences

Proper availability of drug on to corneal surface is a challenging task. However, due to ocular p... more Proper availability of drug on to corneal surface is a challenging task. However, due to ocular physiological barriers, conventional eye drops display poor ocular bioavailability of drugs ( 1%). To improve precorneal residence time and ocular penetration, earlier our group developed and evaluated in situ gel and nanoparticles for ocular delivery. In interest to evaluate the combined effect of in situ gel and nanoparticles on ocular retention, we combined them. We are the first to term this combination as "nanoparticle laden in situ gel", that is, poly lactic co glycolic acid nanoparticle incorporated in chitosan in situ gel for sparfloxacin ophthalmic delivery. The formulation was tested for various physicochemical properties. It showed gelation pH near pH 7.2. The observation of acquired gamma camera images showed good retention over the entire precorneal area for sparfloxacin nanoparticle laden in situ gel (SNG) as compared to marketed formulation. SNG formulation cleared at a very slow rate and remained at corneal surface for longer duration as no radioactivity was observed in systemic circulation. The developed formulation was found to be better in combination and can go up to the clinical evaluation and application.

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Chronicles of Young scientists, Jan 2011

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Cefoperazone sodium impregnated polycaprolactone composite implant for osteomyelitis

Abstract The use of local antibiotics from a biodegradable implant for chronic osteomyelitis is a... more Abstract The use of local antibiotics from a biodegradable implant for chronic osteomyelitis is an attractive alternative. The implant delivers high antibiotic concentration at tissue levels, obliterates dead space, aids bone repair and does not need to be removed. The purpose of this paper is to develop and evaluate a calcium sulphate and polycaprolactone based composite biodegradable implantable delivery system of cefoperazone sodium. Implants were prepared by modified fabrication technique to avoid solvent use.

pH-Induced in situ gel for periodontal anesthesia

Abstract A pH mediated in situ gelling system was developed using prilocaine hydrochloride for pe... more Abstract A pH mediated in situ gelling system was developed using prilocaine hydrochloride for periodontal anesthesia using combination of chitosan and hydroxypropylmethylcellulose. The gel so developed can be used as anaesthetic in lengthy dental surgery. The gel was evaluated for many parameters like gelation pH, viscosity, physicochemical properties, in vitro release, sterility and stability.

Pyrazole incorporated 1, 2-diazanaphthalene derivatives: Synthesis and in-vivo pharmacological screening as anti-inflammatory and analgesic agents

In the present study, a new series of compounds (3 to 22) containing pyrazole moiety clubbed with... more In the present study, a new series of compounds (3 to 22) containing pyrazole moiety clubbed with 1, 2-diazanaphthalene ring, structurally related to celecoxib and naproxen was synthesized. The compounds were evaluated for anti-inflammatory activity using carrageenan induced rat paw edema bioassay. Compounds showing marked anti-inflammatory activity were further tested for their analgesic, ulcerogenic and lipid peroxidation effect using naproxen as reference drug.

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Two faces of carbon nanotube: toxicities and pharmaceutical applications

Critical reviews in therapeutic drug carrier …, Jan 1, 2012

In the field of nanotechnology, carbon nanotube (CNT) is gaining importance for the delivery of t... more In the field of nanotechnology, carbon nanotube (CNT) is gaining importance for the delivery of therapeutic agents and diagnosis of diseases. CNT is emerging as an efficient nanocarrier system with cylindrical nanostructure. Due to its nanoscale dimensions, CNTs have a high cell-penetration quality that allows its use in site-specific targeting. Another aspect of the utilization of CNT lies in its hollow structure through which an active moiety can be delivered in a controlled manner via CNTs' nano channels. Despite these positive aspects of CNT, scientists are still working to improve its biocompatibility and solubility and eliminating toxicity in vivo, which are creating problems with the use of CNTs. Therefore, functionalization becomes an important aspect to be studied because it decreases the toxicity of CNTs and make them nonimmunogenic. In this review, different functionalization techniques of CNTs and their biomedical applications-in particular for cancer therapy to date-are reviewed in detail to present the potential of this nanovector.

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Contact lenses in ocular therapeutics

Drug discovery today, Jan 1, 2012

Drug delivery is a difficult task in the field of ocular therapeutics. Owing to the physiological... more Drug delivery is a difficult task in the field of ocular therapeutics. Owing to the physiological and anatomical constraints of the eye, it is difficult to obtain the correct therapeutic concentration of a drug at the required site of action. This has led to clinicians recommending frequent dosing, which has resulted in noncompliance by patients and decreased cost effectiveness. To overcome these barriers, scientists have explored novel ocular delivery systems, such as in situ gels, ocuserts, nanoparticles and liposomes. A particularly novel form of such a delivery system are contact lenses, which are thin, curved plastic disks that are designed to cover the cornea and which cling to the surface of the eye owing to surface tension. In this article, we describe the introductory literature on ocular delivery using contact lenses, their classification and manufacturing process, and recent advances on drug delivery techniques using such lenses.

Parenteral drug delivery: a review

The parenteral route of administration is the most effective route for the delivery of the active... more The parenteral route of administration is the most effective route for the delivery of the active pharmaceutical substances with narrow therapeutic index, poor bioavailability especially for those drugs, prescribed to unconscious patients. To maintain a therapeutic effective concentration of the drug, it requires frequent injections which ultimately lead to patient discomfort. In parenteral drug delivery, major progress has been done in the field of formulation technologies so as to provide a targeted and sustained release of drug in predictable manner. The present article reviews recent patents and major advancements in parenteral drug delivery systems along with general introduction. This article also deals with importance of novel systems in drug delivery to overcome the problems associated with conventional parenteral drug delivery systems.

Recent Trends in Oral Drug Delivery: A Review

There are many ways to deliver drugs into the body, viz oral (through swallowing), sub mucosal (t... more There are many ways to deliver drugs into the body, viz oral (through swallowing), sub mucosal (through buccal and sublingual mucosa), parenteral (through injection), transdermal (through skin), pulmonary (through inhalation) etc. Among these deliveries oral delivery (by swallowing) is widely accepted. In oral drug delivery, many scientific challenges and breakthrough technologies are required to generate novel dosage forms raising drug delivery to higher level. Some are self emulsifying systems, solid self nanoemulsion, polymeric micelles, spray freezing, pH controlled systems, time delayed system, osmotic pumps, prodrugs etc. This paper reviews recent patents, technologies and products with their importance, manufacturing and novel approaches implemented till date to overcome the challenges in oral drug delivery systems.

Spectrophotometric methods for the estimation of mycophenolate mofetil

An attempt was made to develop and validate a novel, simple, cost effective, accurate, and reprod... more An attempt was made to develop and validate a novel, simple, cost effective, accurate, and reproducible UV-spectrophotometric method to estimate mycophenolate mofetil in bulk and pharmaceutical formulations. Mycophenolate mofetil was estimated at 250 nm in 0.1N hydrochloric acid (pH 1.2) and in acetate buffer (pH 4.5). Beer’s law was obeyed in the concentration range of 5–40 μg/ml in hydrochloric acid and in the acetate buffer medium. The methods were tested and validated for various parameters according to ICH guidelines. The proposed methods were successfully applied for the determination of mycophenolate mofetil in pharmaceutical formulations (tablets and capsules). The results demonstrate that the procedure is accurate, precise, and reproducible (relative standard deviation <2%) while being simple, cheap, and less time-consuming, and hence can be suitably applied for the estimation of mycophenolate mofetil in different dosage forms and for dissolution studies.

Fabrication of cefuroxime-impregnated calcium sulfate: Polycaprolactone composite implant for osteomyelitis

E-Tongue: A Tool for Taste Evaluation

Taste has an important role in the development of oral pharmaceuticals. With respect to patient a... more Taste has an important role in the development of oral pharmaceuticals. With respect to patient acceptability and compliance, taste is one of the prime factors determining the market penetration and commercial success of oral formulations, especially in pediatric medicine. Taste assessment is one important quality-control parameter for evaluating taste-masked formulations. Hence, pharmaceutical industries invest time, money and resources into developing palatable and pleasant-tasting products. The primary method for the taste measurement of a drug substance or a formulation is by human sensory evaluation, in which tasting a sample is relayed to inspectors. However, this method is impractical for early stage drug development because the test in humans is expensive and the taste of a drug candidate may not be important to the final product. Therefore, taste-sensing analytical devices, which can detect tastes, have been replacing the taste panelists. In the present review we are presenting different aspect of electronic tongue. The review article also discussed some useful patents and instrument with respect to E-tongue.

Biological Activities of Pyrazoline Derivatives -A Recent Development

Pyrazolines are well known and important nitrogen containing 5-membered heterocyclic compounds an... more Pyrazolines are well known and important nitrogen containing 5-membered heterocyclic compounds and various methods have been worked out for their synthesis. Numerous pyrazoline derivatives have been found to possess considerable biological activities, which stimulated the research activity in this field. They have several prominent effects, such as antimicrobial, antimycobacterial, antifungal, antiamoebic, anti-inflammatory, analgesic, antidepressant and anticancer activities. They also possess some potent receptor selective biological activity like Nitric oxide synthase (NOS) inhibitor and Cannabinoid CB1 receptor antagonists activity. 4,5-dihydro-1H- pyrazolines seem to be the most frequently studied pyrazoline type compounds. As a result, a large number of such pyrazolines using different synthetic methods for their preparation have been described in the chemistry literature. The present review provides an insight view to pyrazolines synthesis and its biological activities along with the compilation of recent patents on pyrazolines.

Synthesis, Antidepressant and Antifungal Evaluation of Novel 2-Chloro-8-methylquinoline amine Derivatives

A new series of N-[(2-chloro-8-methylquinolin-3-yl)methyl]-(substituted)-aniline / butylamine / c... more A new series of N-[(2-chloro-8-methylquinolin-3-yl)methyl]-(substituted)-aniline / butylamine / cyclohexylamine / benzylamine derivatives (4a-p) was synthesized by nucleophilic substitution reaction of 2-chloro-3-(chloromethyl)-8-methylquinoline 3 with various aliphatic and aromatic amines in absolute ethanol in the presence of triethylamine (TEA). The newly synthesized secondary amines were characterized by combined use of IR, 1H-NMR, 13C-NMR, mass spectral data and microanalyses. The antidepressant activity of the synthesized compounds (4a-p) was evaluated by Forced swim test in rats and their neurotoxicity was evaluated by the rotarod test. Test compounds and clomipramine were administered intraperitoneally at dose of 100 mg/kg and 20 mg/kg respectively. Preliminary antidepressant screening of compounds (4a-p) revealed that compounds 4b, 4c, 4d, 4e, 4i and 4o significantly (P<0.01) reduces the duration of immobility time. These compounds were also tested in-vitro for MAO inhibitory effect. All the compounds were also screened for antifungal activity against Aspergillus niger MTCC 281, Aspergillus flavus MTCC 277, Monascus purpureus MTCC 369 and Penicillium citrinum NCIM 768 strains.

Biological Activities of Quinoline Derivatives

Quinoline and its fused heterocyclic derivatives tested with diverse pharmacological activity con... more Quinoline and its fused heterocyclic derivatives tested with diverse pharmacological activity constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. The present review provides an in depth view of work done so far on quinolines and its biological activities covering anticancer, antimycobacterial, antimicrobial, anticonvulsant, antiinflamatory and cardiovascular activities.

Molecular modeling

The use of computational chemistry in the development of novel pharmaceuticals is becoming an inc... more The use of computational chemistry in the development of novel pharmaceuticals is becoming an increasingly important tool. In the past, drugs were simply screened for effectiveness. The recent advances in computing power and the exponential growth of the knowledge of protein structures have made it possible for organic compounds to be tailored to decrease the harmful side effects and increase the potency. This article provides a detailed description of the techniques employed in molecular modeling. Molecular modeling is a rapidly developing discipline, and has been supported by the dramatic improvements in computer hardware and software in recent years.

Patent protection strategies

It is widely recognized that the pharmaceutical industry faces serious financial challenges. Larg... more It is widely recognized that the pharmaceutical industry faces serious financial challenges. Large numbers of blockbuster drugs are losing patent protection and going generic. The pipeline of new drugs is too sparse to fill the gap and generate a platform for future growth. Moreover, many of the new products are biologics with much narrower target patient populations and comparatively higher prices relative to traditional pharmaceuticals. So now the time has come for pharmaceutical scientists to have a better understanding of patent fundamentals. This need is illustrated by analyses of key scientific and legal issues that arose during recent patent infringement cases involving Prozac, Prilosec, and Buspar. Facing this scenario, the pharmaceutical industry has moved to accelerate drug development process and to adopt at the same time different strategies to extend the life time of the patent monopoly to provide the economic incentives and utilizing it for drug discovery and development. This review covers the need of patent protection and various strategies to extend the patent.

Isolation and purification of fungal pathogen (Macrophomina phaseolina) induced chitinase from moth beans (Phaseolus aconitifolius)

Objective : Chitinase (EC 3.2.1.14) is one of the major pathogenesis-related proteins, which is a... more Objective : Chitinase (EC 3.2.1.14) is one of the major pathogenesis-related proteins, which is a polypeptide that accumulates extracellularly in infected plant tissue. An attempt was made to isolate and purify the chitanase enzyme using moth beans as an enzyme source. Materials and Method : The enzyme was isolated and purified from moth beans against the fungal pathogen Macrophomina phaseolina strain 2165. The isolation and purification was done in both in vitro and in vivo conditions. Purification of chitinase was carried out to obtain three fractions, viz. 50°C heated, ammonium sulfate precipitated and sephadex G-25 column-eluted fractions. The molecular mass of Chitinase was directly estimated by sodium dodecyl sulfate-polyacryamide gel electroresis (SDS-PAGE). Result : The yield is sufficient for initial characterization studies of the enzyme. The molecular study of the enzyme shows the possibility of generating the defense mechanism in plants in which it cannot occur. Chitinase was purified by gel filtration chromatography with 20.75-fold and 32.78-fold purification in the in vitro and in vivo conditions, respectively. The enzyme shows a maximum activity after 90 min with 0.1 ml of colloidal chitin as a substrate and 0.4 ml of crude chitinase extract. The optimum pH of 5.0 and an optimum temperature of 40°C was found for maximal activity. The molecular weight of purified chitinase was estimated to be 30 kDa by SDS-PAGE. Conclusion : The chitinase isolated in both in vitro and in vivo conditions is stable andactive.