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

Objective: Chlorzoxazone (CLZ) is centrally acting skeletal muscle relaxant. It is insoluble in water, so employed for the formation of solid dispersions (SD) as a means to enhance the dissolution rate and carrier selected was polyethylene glycol 6000 (PEG 6000). Methods: The SDs were prepared by different methods and characterized by in vitro drug release, drug content, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, powder X-ray diffraction. All the SD showed dissolution improvement compare to pure drug. These techniques revealed distinct loss of drug crystallinity in the formulation accounting for enhancement in dissolution rate. The SD methods showing best in vitro drug release profile were selected in the further development of mucoadhesive buccal patches. A buccal patch has been developed using two mucoadhesive polymers, i.e. hydroxyl propyl methyl cellulose K4M and carbopol 974. The patches were evaluated for the physicochemical, mechanical and drug release characteristics. The optimized patches showed good mechanical and physicochemical properties to withstand the environment of the oral cavity. The in-vitro permeation study showed that patches could deliver drug to the oral mucosa for a period of 8 hrs. Results: The results indicate that suitable bioadhesive buccal patches with good permeability could be prepared. The batches FH4 and FC4 showed 81.95% and 79.97% permeated through goat mucosa membrane in 8 hrs. The physicochemical interactions were investigated by FTIR, showed no any evidence of interactions and were present in an unchanged state. The stability study for SD and buccal patch carried out revealed that were stable for a period of 3-month. Conclusion: Phase-solubility studies indicate significantly increase in solubility. The optimized buccal patches showed good mechanical and physicochemical properties to withstand environment of the oral cavity.

World University root node

Pharmacy

Asian Journal of Pharmaceutical and Clinical Research

Development of mucoadhesive delivery of chlorzoxazone polyethylene glycol solid dispersion

Background 6-MP has short elimination time (<2 h) and low bioavailability (~ 50%). Present study was aimed to develop time controlled and site targeted delivery of 6-Mercaptopurine (6-MP) for treatment of colon diseases. Methods: Compression coating technique was used. 32 full factorial design was designed for optimization of the outer coat for the core tablet. For outer coat amount of Eudragit RS 100 and hydroxypropyl methylcellulose (HPMC K100) were employed as independent variables each at three levels while responses evaluated were swelling index and bursting time. Direct compression method was used for tablets formulation. Results: 80% w/w of microcrystalline cellulose and 20% w/w of croscarmellose sodium were found to be optimum concentration for the core tablet. The outer coat of optimized batch (ED) contains 21.05% w/w Eudragit RS 100 and 78.95% w/w HPMC K100 of total polymer weight. In-vitro dissolution study indicated that combination of polymer retards the drug release in gastric region and releases ≥95% of drug in colonic region after ≥7 h. Whereas in case of in-vivo placebo x-ray imaging study had shown that the tablet reaches colonic part after 5±0.5 h providing the proof of arrival in the colon. Stability study indicated that the optimized formulation were physically and chemically stable. Conclusion: Present research work concluded that compression coating by Eudragit RS 100 and HPMC K100 to 6-MP core provides potential colon targeted system with advantages of reduced gastric exposure and enhanced bioavailability. Formulation can be considered as potential and promising candidate for the treatment of colon diseases. © 2016 Bentham Science Publishers.

Current Drug Delivery

Optimization of Time Controlled 6-mercaptopurine Delivery for Site- Specific Targeting to Colon Diseases

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$\alpha$ amylase and $\alpha$ glucosidase inhibitory activities and HPTLC fingerprinting analysis of methanolic extract of Citrullus lanatus seeds

The present study was planned to investigate the effect of polymer composites HPMC K15 M and poloxamer 407 on developed dorzolamide hydrochloride in situ gel. Formulations were prepared based on 32 factorial design with concentrations of Poloxamer 407 and HPMC K15 M as independent variables. Gelation temperature, viscosity study at 37 °C and % cumulative drug release upto 8 h were considered as dependent variables. Polymer composites showed linear model with gelation temperature and quadratic model with viscosity study at 37 °C and % cumulative drug release up to 8 h. Optimized formulation successfully sustained release of drug upto 5 h in ex vivo goat corneal permeability study. Comparative in vivo study in normotensive rabbits showed that optimized formulation sustained therapeutic effect upto 8 h with 31.22 ± 3.65% reduction in intraocular pressure and marketed formulation showed immediate release effect with 18.22 ± 4.42% reduction in intraocular pressure upto 2-3 h.

Journal of Drug Delivery Science and Technology

Influence of hydroxypropylmethylcellulose and poloxamer composite on developed ophthalmic in situ gel: Ex vivo and in vivo characterization

{\textcopyright} 2016 Bentham Science Publishers.The Objective of the present work was to enhance the solubility and dissolution profile of poorly water soluble BCS class II drug Tinidazole (TNZ). Microwave energy was utilized to prepare solvent free solid dispersions of TNZ and combination of TNZ with hydrophilic carriers as urea, gum acacia, $\beta$ cyclodextrin ($\beta$ CD), polyethylene glycol 6000 and polyvinyl pyrolidone Formulated solid dispersions were characterized by FTIR, solubility, microscopy, melting point and physical characterization by DSC and PXRD. Results revealed principal peak values in FTIR spectra of the drug remain unchanged in microwave-induced solid dispersions indicating no chemical interaction. Enhancement of solubility in microwave irradiated TNZ ranged from 7.52% to 55.02%, while for MSD TNZ: Urea it enhances from 9.70% to 86.82%. This may be due to conversion of crystalline to amorphous form, which was confirmed by differential scanning calorimetry and powder X-ray diffraction. Dissolution profile of the microwave irradiated TNZ enhanced by 22% and that of MSD TNZ: Urea by 25%. TNZ was interacted with $\beta$-CD and the docking enrgy was found to be -9.4558 kcal/mol. Binding energies of complex (TNZ: $\beta$-CD) has shown favourable electrostatic interaction. It was found that binding energies decrease after docking indicating stability of $\beta$-CD-TNZ complex.

Letters in Drug Design & Discovery

Design and evaluation of microwave induced solid dispersion of tinidazole and molecular modelling with β-cyclodextrin

Objective: To develop and validate stability indicating HPTLC method for simultaneous quantitative determination of candesartan cilexetil (CDT) and hydrochlorothiazide (HCT) in pharmaceutical dosage form. Methods: The present study deals with development and validation of stability indicating HPTLC method for simultaneous estimation of CDT and HCT. Chromatographic separation was performed on aluminum plate precoated with Silica Gel 60 F254 using toluene: chloroform: ethanol: glacial acetic acid (2:7:1:0.1 v/v) as mobile phase. The wavelength selected for densitometry scanning was 270 nm. Regression plots revealed linear relationships in the concentration range of 500-5000 and 400-2000 ng/band for CDT and HCT respectively. The correlation coefficient of calibration curves was found to be more than 0.99 for both analytes. Results: The chromatographic conditions gave compact spots at Rf value (±SD) 0.12 (±0.01) and 0.70 (±0.02) for HCT and CDT respectively. The method was validated as per International Conference on Harmonization (ICH) guidelines, demonstrating to be accurate and precise within the corresponding linearity range of titled analytes. Inherent stability of these drugs was studied by exposing drug substances to various stress conditions as per ICH guidelines namely oxidative, photolysis and hydrolytic conditions under different pH. Relevant degradation was found to take place under these conditions. Conclusion: A new simple, accurate, precise, sensitive and economic stability-indicating HPTLC method has been developed and validated for the simultaneous determination of CDT and HCT in pharmaceutical dosage form. The proposed method can be used for the routine estimation of CDT and HCT in bulk and formulation and can be employed for stability-indicating analysis.

International Journal of Pharmacy and Pharmaceutical Sciences

Application of a validated stability-indicating hptlc method for simultaneous quantitative determination of Candesartan cilexetil and hydrochlorothiazide in pharmaceutical dosage form

Zolmitriptan is the drug of choice for the treatment of migraine with or without aura. Oral bioavailability of drug is 40% due to high first pass metabolism. Elimination half life is 3 hrs and drug degradation occurs in acidic environment of GIT. To overcome these problems present research was aimed to prepare intestinal targeted delivery. This was prepared by compression coating technique as maximum absorption of drug occurs in small intestine. 32 factorial design was applied with independent variables polyox N12K and methacrylic acid. Core tablet consists of croscarmellose sodium as superdisintegrant, avicel as binder, dicalcium phosphate as diluent and zolmitriptan as drug. Outer coating of polyox N12K and methacrylic acid was applied in compression coating. Optimized batch F8 consist of polyox N12K (60%) & methacrylic acid (3%). In-vitro release study in simulated media indicated presence of the tablet in small intestine giving burst release. In-vivo placebo X- ray radiographic technique for F8 showed that tablet was not adhered throughout GIT and bypass stomach. This indicated F8 can be a potential to achieve the targeted site delivery.

Current Drug Therapy

Optimization of Site Targeted Zolmitriptan Delivery Using Polyox N12K and Methacrylic Acid

Nasal route had shown better systemic bioavailability due to its large surface area, porous endothelial membrane, high total blood flow and avoidance of first-pass metabolism. Timolol maleate is a beta blocker used primarily in the treatment of hypertension. Drug undergoes extensive hepatic first-pass metabolism (80%). The drug has half-life of 4 hrs. Oral bioavailability of timolol maleate is 61%. The aim of the present study was to optimize controlled release in situ nasal delivery for timolol maleate. HPMC and Poloxamer 407 were selected as polymer in formulation of thermoreversible in situ nasal gel. Optimization was carried out using 32 factorial design. It was observed that formulations f1 and f4 revealed the highest % drug release, that is, 93.57% and 91.66%, respectively. Factorial design study indicated that the drug release and viscosity were most significant dependent factors. Ex vivo diffusion study through nasal mucosa indicated 67.26 ± 2.10% and 61.07 ± 2.49% drug release for f1 and f4 formulations. f1 was the optimized batch. This batch thus can act as a potential nasal delivery with enhanced bioavailability for the drug.

Fulltext

Scientifica

Optimization of Thermoreversible in Situ Nasal Gel of Timolol Maleate

Objective: The present work describes stability indicating (SI) RP-HPLC-PDA method for determination of abiraterone acetate (ABA) and characterization of its base catalyzed degradation product by LC-MS. Methods: The separation was achieved by using column Kromasil C18 (250 mm x 4.6 mm, 4.0 µ) using acetonitrile (ACN): ammonium acetate buffer 10 mM, pH adjusted to 3.5 with acetic acid (AA) in the ratio of 10:90 % v/v as eluent. The Mobile phase flow rate was 0.6 ml/min and data integration was achieved at 235 nm. Results: The retention time of ABA was 5.4±0.01 min. Linearity was found to be in the range of 5-30 µg/ml. The limit of detection and quantitation were 0.25 µg/ml and 0.75 µg/ml respectively and percentage recovery of ABA was found to be 99.52 to 100.13 %. Mass spectral data of base degraded product of ABA shows a prominent molecular ion peak at m/z-391.5. Major fragmentation leads to formation of 10-Methyl 2,3,4,7,8,9,10,11,12,13,14,15-dodecanhydro-1H cyclopenta (a)phenanthren-3-ol as a degradant (D2) at m/z-257.81, due to corresponding loss of C8H12ON. All the analytical validation parameters were determined and found in the limit as per ICH guidelines. Conclusion: The results of the various validation studies showed that the LC method is fast, specific, accurate, reproducible, possessed significant linearity and precision. The drug was found to be stable under all the stress conditions except basic stress. Thus developed method reported first time is novel with a very short run time of 6 min..

Stability indicating RP-HPLC-PDA method for determination of abiraterone acetate and characterization of its base catalyzed degradation product by LC-MS

Seventeen (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 one derivatives were synthesized via aldol condensation of substituted benzaldehydes with quinoline chalcones starting from 8-hydroxy quinoline. Molecular docking studies were performed on COX-2 protein for analgesic activity and PDE 4 enzyme for anti-asthmatic activity. Docking studies for analgesic activity reveal that the compounds 2, 4, 12, 14, and 15 showed significant interaction in terms of hydrogen bonding, hydrophobic attachment and van der Waal interaction with COX-2. The docking studies and pharmacological screening indicate that substitution of hydroxyl and conjugated ketone groups on the aldehyde ring and the quinoline ring accelerates analgesia with better binding to active site. Eddy's hot plate method was used to evaluate analgesic activity of the synthesized compounds. Compounds showed a substantial increase in reaction time when compared with standard pentazocin. Compounds 2, 4, 7, 9 and 13 showed significant binding interactions with PDE 4 enzyme and hence were selected for evaluation of anti-asthmatic activity using the goat tracheal chain method. Studies reveal that substitution of the methoxy group at 4th &amp; 5th positions for compounds 2, 4 &amp; 7 leads to significant percentage inhibition of histamine induced contraction. The synthesized compounds are thus found to be potent as analgesic and anti-asthmatic agents. © 2014 The Authors

Arabian Journal of Chemistry

Synthesis and evaluation of analgesic, anti-asthmatic activity of (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 ones Synthesis, evaluation, analgesic anti-asthmatic activity of (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 one