MIT-World Peace University (MIT-WPU) is a top educational institute located in Pune, India. It is recognized within&nbsp;UGC under Government of Maharashtra Act No. XXXV 2017.&nbsp;

It is part of the MIT group of institutions (established in 1983) which covers 10+ campuses across India and has more than 50,000+ students enrolled across various disciplines at a given point of time. The institute houses 15 schools ranging from Engineering &amp; Technology, Design, Pharmacy, Commerce, Governance among others. It offers undergraduate, postgraduate and PhD programs among different disciplines.&nbsp;

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MIT World Peace University

School of Pharmacy

BACKGROUND: Triamcinolone is a long acting corticosteroid used in the treatment of arthritis, eczema, psoriasis and similar conditions which cause inflammation. Triamcinolone has half-life of 88min. Prolonged oral use is associated with gastrointestinal adverse effects as peptic ulcer, abdominal distention and ulcerative esophagitis as described in various patents. Microemulgel offers advantage of better stability, better loading capacity and controlled release especially for drug with short half life. OBJECTIVE: Objective of the present study was to optimize microemulgel based transdermal delivery of triamcinolone. METHOD: Saturated solubility of triamcinolone in various oils, surfactants and co-surfactants is estimated. Pseudo-ternary phase diagrams were constructed to determine the region of transparent microemulsion. Microemulsion was evaluated for globule size (FE-SEM, zetasizer), % transmittance, pH, viscosity, conductivity etc. Design of experiment was used to optimize microemulsion based gel. Carbopol 971P and HPMC K100M were used as independent variables. Microemulsion based gel was evaluated for in-vitro as well as ex-vivo parameters. RESULTS: Microemulsion was formulated with oleic acid, lauroglycol FCC and propylene glycol. PDI 0.197 indicated microemulsion is mono-disperse. 32 factorial design gave batch F8 as optimized. Design expert suggested drug release; gel viscosity and bio-adhesive strength were three significant dependant factors affecting the transdermal delivery. F8 showed drug release 92.62.16±1.22% through egg membrane, 95.23±1.44% through goat skin after 8hr and Korsmeyer-Peppas release model was followed. CONCLUSION: It can be concluded that a stable, effective controlled release transdermal microemulgel was optimised for triamcinolone. This would be a promising tool to deliver triamcinolone with enhanced bioavailability and reduced dosing frequency.

Pharmacy

World University root node

Recent Patents on Anti-Infective Drug Discovery

Optimization of Microemulsion Based Transdermal Gel of Triamcinolone

The present work reports the synthesis and evaluation of antimicrobial activity of polyindole–TiO2 nanocomposite. Polyindole–TiO2 nanocomposite was synthesized by aqueous in situ chemical polymerization of indole using ammonium persulfate as an oxidant under ultrasonic condition. The synthesized polyindole and polyindole–TiO2 nanocomposites were characterized by ultraviolet-visible spectroscopy, Fourier transform infrared spectroscopy, scanning electron microscope, thermogravimetric analysis and X-ray diffraction techniques. A sharp peak at ∼1,402 cm−1 is due to the stretching vibrations of O‒Ti‒O bond in polyindole–TiO2 nanocomposite. The X-ray diffraction pattern shows the major diffraction peaks at 25°C and 48°C, indicating TiO2 in anatase form. Polyindole–TiO2 shows maximum activity against gram-positive Staphylococcus aureus and Bacillus subtilis as compared to gram-negative Escherichia coli.

Polymer - Plastics Technology and Engineering

Ultrasound Synthesis of Polyindole–TiO2 Nanocomposite and Evaluation of Antibacterial Activity

Purpose: Ofloxacin is a fluoroquinolone with broad-spectrum antibacterial action, used in treatment of systemic and local infections. Ofloxacin is BCS class II drug having low solubility, high permeability with short half-life. The present work was aimed to design, develop and optimize gellified emulsion of Ofloxacin to provide site targeted drug delivery. Transdermal drug delivery will enhance the bioavailability of the drug giving controlled drug release. Methods: Transdermal drug delivery system was designed with gelling agent (Carbopol 940 and HPMC K100M), oil phase (oleic acid) and emulsifying agent (Tween 80: Span 80). Effect of concentration of gelling agent on release of drug from transdermal delivery was studied by 32 factorial design. Emulgel was evaluated for physical appearance, pH, drug content, viscosity, spreadability, antimicrobial activity, in- vitro diffusion study and ex-vivo diffusion study. Results: FE-SEM study of the emulsion batch B5 has revealed formation of emulsion globules of approximately size 6-8 $\mu$m with -11.2 mV zeta potential showing good stability for the emulsion. Carbopol 940 had shown greater linear effect on drug release and viscosity of the formulations due to its high degree of gelling. In-vitro diffusion study through egg membrane had shown 88.58±1.82 % drug release for optimized batch F4. Exvivo diffusion study through goat skin indicated 76.68 ± 2.52% drug release. Conclusion: Controlled release Ofloxacin emulgel exhibiting good in-vitro and ex-vivo drug release proving good antimicrobial property was formulated.

Fulltext

Advanced Pharmaceutical Bulletin

Gellified emulsion of Ofloxacin for transdermal drug delivery system

The methanolic whole plant extract of Biophytum sensitivum (感应草gǎny{\`{i}}ng cǎo) has been found to possess antiurolithiatic effect. The present study was undertaken to evaluate the antiurolithiatic effect of some fractions of methanolic whole plant extract of B. sensitivum (MBS) in rats as a step toward activity-directed isolation of antiurolithiatic component. The MBS was successively extracted with dichloromethane, ethyl acetate, ethanol and water to obtain fractions. Sodium oxalate (70 mg/kg, i.p.) was administered to rats for seven days to develop calcium oxalate urolithiasis. These rats were treated with two doses (20 and 40 mg/kg, p.o.) of the fractions, 1 h before sodium oxalate injections. Antiurolithiatic activity was assessed by estimating biochemical changes in urine, serum and kidney homogenate along with histological changes in kidney tissue. Sodium oxalate administration caused biochemical alterations in urine which was found to be prevented significantly by the ethyl acetate fraction. Supplementation with ethyl acetate fraction prevented the elevation of serum creatinine, uric acid and blood urea nitrogen levels. The elevated calcium, oxalate and phosphate levels in the kidney tissue homogenate of lithiatic rats were significantly reduced by the treatment with ethyl acetate fraction. The ethyl acetate fraction also caused significant decrease in lipid peroxidation activity, accumulation of calcium oxalate deposits and histological changes in the kidney tissue. The results showed that the antiurolithiatic component of the methanolic whole plant extract of the plant is contained in the ethyl acetate fraction. The effect is attributed to its diuretic, antioxidant, nephroprotective properties and effect on lowering the concentration of urinary stone-forming constituents.

Journal of Traditional and Complementary Medicine

Protective effect of ethyl acetate fraction of Biophytum sensitivum extract against sodium oxalate-induced urolithiasis in rats

A facile, green approach for the synthesis of some new dibenz[1,4]-diazepine-1-one by a three component reaction of Diamine, 1,3 diketone and aromatic aldehyde using oxalic acid as catalyst in water is described. The products are formed in good yields (92–94%). Newly synthesized dibenz [1,4]-diazepine-1-one analogues were evaluated for the anxiolytic activity by the elevated plus maze method. From the activity data it is observed that compounds, 4g, 4h and 4k show promising anxiolytic activity.

Arabian Journal of Chemistry

Green synthesis and anxiolytic activity of some new dibenz-[1,4] diazepine-1-one analogues

Purpose: Inflammatory bowel disease (IBD) is a chronic, relapsing and often life-long disorder. The best way to tackle IBD is to develop a site targeted drug delivery. Methylprednisolone is a potent anti-inflammatory steroid. The relative potency of methylprednisolone to hydrocortisone is at least four is to one. The aim of the present research was to develop a colon targeted drug delivery for treatment of IBD. Methods: Compression coated drug delivery system was designed and optimised. Core tablet contained drug, croscarmellose sodium (CCS-superdisintegrant), avicel (binder) and dicalcium phosphate (diluent). Design of experiment with 32 factorial design was applied for optimization of compression coated delivery. Chitosan and cellulose acetate phthalate were chosen as independent variables. Swelling index, hardness and % drug release were dependant variables. Results: Core tablet (C5 batch) containing 2.15% CCS showed disintegration in less than 10sec. FTIR, UV and DSC study had shown absence of any significant physical and chemical interaction between drug and polymers. F8 was found to be optimised formulation. F8 contained 35% chitosan and 17.5% cellulose acetate phthalate. It showed drug release of 86.3% ± 6.1%, hardness 6.5 ± 1.5 and lag time 7 hrs. Simulated media drug release was 97.51 ± 8.6% with 7.5 hrs lag time. The results confirmed that the lag time was highly affected by the coating of the polymers as well as the concentration of the superdisintegrant used in core tablet. Conclusion: In-vitro and in-vivo results confirmed a potential colon targeted drug therapy for treatment of IBD.

Optimization of chitosan and cellulose acetate phthalate controlled delivery of methylprednisolone for treatment of inflammatory bowel disease

Background: Inflammatory bowel disease (IBD) is one of the five most prevalent gastrointestinal disease burdens which commonly require lifetime care. Worldwide incidence rate of ulcerative colitis and Crohn's disease is about 16.8% and 13.4% respectively. Colitis is an inflammation of the colon. Colon targeted drug delivery will direct the drug to the colon. The drug will reach at the site of action and hence its side effects as well as dose can be reduced. Recent patent describes treatment of ulcerative colitis using anti CD3 antibodies, with nicotine and anti-depressant drugs, budesonide foam etc. Objective: Present study deals with optimization of site targeted methylprednisolone delivery for treatment of colitis. Method: Chitosan and Eudragit RS 100 were used as coating polymers. Tablets were prepared by press coated technology. The core tablets contain drug, avicel as binder, croscarmellose sodium as super disintegrant and dicalcium phosphate as diluent. Drug excipient compatibility was carried out using FTIR, UV and DSC. Design of experiment was used to optimize the formulation. Tablets were evaluated for thickness, weight variation, hardness, swelling index, in-vitro drug release and release of drug in simulated media. Results: Optimized batch (B2) contained chitosan 40% and eudragit RS 100 17.5%. B2 showed in-vitro drug release 85.65 ± 7.6% in 6.8 pH phosphate buffer and 96.7 ±9.1% in simulated media after 7.5 hours. Conclusion: In-vivo x-ray placebo study for formulation B2 had shown that the tablet reached to the ascending colon after 5 hours. This indicated a potential site targeted delivery of optimized batch B2. {\textcopyright} 2016 Bentham Science Publishers.

Site Targeted Press Coated Delivery of Methylprednisolone Using Eudragit RS 100 and Chitosan for Treatment of Colitis

In the current trend various regulatory authorities like ICH, USFDA, Canadian Drug and Health Agency are emphasizing on the identification and quantitation of impurities in Active Pharmaceutical Ingredient's (API's) and it is now emerging as a mandatory requirement for the new drug application. Hence their level should be controlled and monitored. Thus a simple sensitive High performance thin layer chromatographic (HPTLC) method for estimation of Propyl thiouracil and its process related impurities has been developed. Propyl thiouracil and its impurities were separated and identified on silica Gel 60 F254TLC plates with Hexane: Acetone: Ethyl Acetate: Formic acid 6:4:1:0.5 (v/v) as mobile phase. The plates were developed to a distance of 8 cm and quantification was performed at $\lambda$ = 254 nm. The method was validated for linearity, accuracy, precision and robustness according to ICH guidelines. The calibration plots were linear in the range 2500-5625 and 50-112.5 ng/band for API and its three impurities respectively. Here recovery value for API and impurities were found to be in the range of 99.99 to 100.75 % with % RSD value always less than 2. Hence the developed method was found to be simple, sensitive, accurate and precise which can be used for propyl thiouracil impurity profile study and for routine analysis of propyl thiouracil from its dosage forms and for IPQC study during manufacturing of its formulations.

International Journal of Pharmaceutical Sciences Review and Research

A validated HPTLC method for determination of propyl thiouracil in the presence of its impurities

Prochlorperazine maleate, a well known antiemetic is used in the treatment and prevention of nausea and vomiting. The dosage of the drug is usually 5 or 10 mg thrice or four times a day, because of its short biological half life (6-8 hours). The bioavailability of drug is 12.5%. Due to the solubility of drug in acidic pH, the drug is absorbed rapidly from stomach. Present study was aimed to formulate and evaluate effervescent floating matrix tablets of Prochlorperazine maleate. Hydroxyethyl cellulose HHX (Natrosol HHX) and hydroxypropyl cellulose (HPC-H) were used as release retarding agents. Sodium bicarbonate and citric acid were used as gas forming agents. Floating tablet of prochlorperazine maleate was prepared to enhance the bioavailability of drug, to prolong the gastric retention time (GRT) and to reduce the frequency of administration. The formulations were prepared by direct compression method. The tablets were evaluated for pre-compression and post-compression parameters. 32 full factorial designs were used to optimize the concentration of release retarding agents. From the factorial batches, formulation H7 containing 70% of hydroxyethyl cellulose HHX and 12% hydroxypropyl cellulose - H was found to be the optimized batch. Formulation H7 followed Korsmeyer Peppas release kinetics, with sustained drug release of 93.64±6.4 % and floating for 10 hours. In-vivo X-ray placebo study of optimized batch (H7) showed retention of tablet in stomach for 6±0.5 hours. Thus, the study proved the successful floating delivery of drug in stomach. © 2016 Bentham Science Publishers.

Current Drug Therapy

Optimization of Natrosol HHX and HPC-H Controlled Floating Delivery for Prochlorperazine Maleate

The Asian tsunami of 26th December, 2004 took the lives of 2,20,000 people and devastated coastal structures, including many thousands of brick-built homes. Many economically backward people who have made their homes in non-engineered masonry lost their shelters. Though very high waves of tsunami cannot be resisted, waves comparable to the height of the masonry structures can be tolerated by these structures by implementing simple design techniques which are cost effective and can be implemented without any modern equipment. The present study throws light on the issues related to effect of brick orientation, number of openings, orientation and shape of the structures with respect to possible direction of wave movement and effect of support conditions upon the performance of masonry structures subjected to tsunami loading. It has also been noticed that boundary walls acts as a barrier to reduce the effect on the actual structures. In this context, this study may be helpful in framing design guidelines for improving the performance of non-engineered masonry structures under tsunami loading. © 2016, The Institution of Engineers (India).