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Ige P.P.,R C Patel Institute Of Pharmaceutical Education And Research | Gattani S.,Swami Ramanand Teerth Marathwada University
Polymer - Plastics Technology and Engineering | Year: 2012

Polymeric floating microspheres of metformin hydrochloride were prepared by a modified solvent evaporation method using ethyl cellulose and HPMC K4M. Microspheres were characterized by SEM, particle size, drug content, in vitro swelling, in vitro buoyancy, in vitro drug release and in vivo X-ray imaging. Formulation D exhibited in vitro swelling, about 48.28 ± 1.03% and the desired floating time and with retention in the upper small intestine of rabbits for 8 h and with release for 12 h. We conclude that ethyl cellulose and HPMC K4M at 0.40:1.50 w/w ratios could be an effective carrier for multiparticulate controlled drug delivery. © 2012 Copyright Taylor and Francis Group, LLC.


Mahajan H.S.,R C Patel Institute Of Pharmaceutical Education And Research | Tyagi V.K.,R C Patel Institute Of Pharmaceutical Education And Research | Patil R.R.,R C Patel Institute Of Pharmaceutical Education And Research | Dusunge S.B.,R C Patel Institute Of Pharmaceutical Education And Research
Carbohydrate Polymers | Year: 2013

The objective of present study was to enhance bioadhesive potential of xyloglucan by thiolation. Thiolation of xyloglucan was achieved with esterification with thioglycolic acid. Thiolated xyloglucan was characterized by NMR, DSC, and XRD analysis. Thiolated xyloglucan was determined to possess 4 mmol of thiol groups/g of polymer by Ellman's method. Comparative evaluation of mucoadhesive property of ondansetron containing in situ gel system of xyloglucan and thiolated xyloglucan using sheep nasal mucosa revealed higher ex vivo bioadhesion time of thiolated xyloglucan as compared to xyloglucan. Improved mucoadhesive property of thiolated xyloglucan over the xyloglucan can be attributed to the formation of disulfide bond between mucus and thiolated xyloglucan. Ex vivo permeation study conducted using sheep nasal showed improved drug permeation in formulation based on thiolated xyloglucan. In conclusion, thiolation of xyloglucan improves its bioadhesion and drug permeation without affecting the resultant gel properties. © 2012 Elsevier Ltd.


Zawar L.R.,R C Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,R C Patel Institute Of Pharmaceutical Education And Research
Chemical and Pharmaceutical Bulletin | Year: 2012

The influence of microwave technology on the in vitro dissolution rate and in vivo antihyperglycemic activity of a poorly water soluble drug, repaglinide (RG) was studied. Solid dispersions were prepared by conventional fusion method and microwave method using poloxamer 188. The dispersions were characterized by solubility study, dissolution study, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and scanning electron microscopy (SEM). Microwave generated solid dispersions exhibited remarkable improvement in solubility and dissolution rate compared to that of pure RG. Results of DSC, XRD and SEM study showed conversion of crystalline form of RG to amorphous form. In vivo studies revealed that the microwave generated solid dispersion showed significant improvements in antihyperglycemic activity as compared to RG alone, thus confirming the advantage of improved pharmacological activity of RG by microwave method. In conclusion, microwave method could be considered as simple, efficient and solvent free promising alternative method to prepare solid dispersion of poorly water soluble drug RG with significant enhancement in solubility, dissolution rate and antihyperglycemic activity. © 2012 The Pharmaceutical Society of Japan.


Kamble S.M.,R C Patel Institute Of Pharmaceutical Education And Research | Goyal S.N.,R C Patel Institute Of Pharmaceutical Education And Research | Patil C.R.,R C Patel Institute Of Pharmaceutical Education And Research
RSC Advances | Year: 2014

Chemotherapeutic agents are a mainstay in the treatment of cancer. However, the nonselectivity of cytotoxic anticancer agents results in multiorgan toxicities. Cancer chemotherapy is often associated with toxicities, which can be expensive to manage and may affect the patient quality of life. Very few organ-protective agents like amifostine are proved as adjuvants to cancer chemotherapy. Amifostine protects against a wide range of chemo- and radiotherapy-related toxicities and reduces costs of supportive care. Multifunctional natural compounds like pentacyclic triterpenoids and their semisynthetic derivatives possess organ-protective activities against drug-induced toxicities. Triterpenoids interact with biomolecules involved in the cytotoxicity of chemotherapeutic agents. They also sensitize cancer cells for cytotoxic effect of chemotherapy. Further, pentacyclic triterpenoids themselves possess anticancer activity. The efficacy of pentacyclic triterpenoids as organotropic, anticancer and chemo sensitizers may prove these agents as adjuvant to cancer chemotherapy. The current review focuses on the systematic studies of the multifunctional role of pentacyclic triterpenoids and their derivatives in chemotherapy. Interactions of pentacyclic triterpenoids with molecular targets like nuclear factor erythroid-derived 2-like 2 (NrF2), nuclear factor kappa B (NFκ-B), protein kinase C (PKC), free radical scavenging, and cell longevity pathways that contribute to cytoprotective, anticancer, chemosensitizer and chemopreventive effects have been emphasized. The therapeutic utility of pentacyclic triterpenoids as multifunctional adjuvants in cancer chemotherapy is highlighted. © the Partner Organisations 2014.


Redasani V.K.,R C Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,R C Patel Institute Of Pharmaceutical Education And Research
European Journal of Medicinal Chemistry | Year: 2012

The present works deals with simple and efficient method of improving therapeutic efficacy of racemic ibuprofen by retarding gastrointestinal side effects through masking of carboxylic group chemically. This is achieved by synthesis and evaluation of ester derivatives of ibuprofen as mutual prodrugs with naturally occurring phenolic and alcoholic compounds. Promoieties like menthol; thymol and eugenol were selected with the aim of getting synergistic effect as these are natural analgesic having traditional medicinal values. Prodrugs are found to be highly lipophilic as compared to parent drug. All the prodrugs are found to be highly stable at acidic pH while undergoes hydrolysis at neutral and alkaline pH as indicated by their t1/2 values. Synthesized prodrugs derivatives show increased anti-inflammatory activity that might be attributed to synergistic effect as ibuprofen conjugates to natural analgesics. Ulcer index shows much reduction in gastric ulceration compared to ibuprofen concluding the successful masking of acidic group. © 2012 Elsevier Masson SAS. All rights reserved.


Shingade S.G.,R C Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,R C Patel Institute Of Pharmaceutical Education And Research
Medicinal Chemistry Research | Year: 2013

The Schiff's bases 3a-3h were synthesized by reacting substituted/ unsubstituted aromatic aldehydes 2a-2h with 1-(2-aminoethyl)-piperazine 1. A series of novel aryl-3-(2-piperazin-1-ylethyl)-1,3-thiazolidin-4-one 4a-4h and 3-chloro-1-{2-[4-(chloroacetyl)piperazin-1-yl]ethyl}-4-arylazetidin-2-one 5a-5h were synthesized from the Schiff's bases of 1-(2-aminoethyl)-piperazine 3a-3h. The structures of synthesized compounds were confirmed by analytical (C, H, and N) and spectral (FT-IR, 1H NMR, 13C NMR, and Mass) data. The compounds 4a-4h and 5a-5h were screened for antimicrobial activity. The compounds 4a, 4d, 4f, 4g, 5a, 5d, 5f, and 5g exhibited substantially significant antibacterial as well as antifungal activity. © 2012 Springer Science+Business Media, LLC.


Ige P.P.,R C Patel Institute Of Pharmaceutical Education And Research | Gattani S.G.,H R Patel Institute Of Pharmaceutical Education And Research
Archives of Pharmacal Research | Year: 2012

The aim of the current work was to design and develop matrix pellets of hydroxy propyl methyl cellulose K200M and microcrystalline cellulose in an admixture for a mucoadhesive gastroretentive drug delivery system. Pellets containing metformin hydrochloride (500 mg) were prepared by the pelletization technique using an extruder-spheronizer. Pellets were characterized by differential scanning calorimetry (DSC), x-ray diffraction (XRD), scanning electron microscopy (SEM), circularity, roundness, percent drug content, percent production yield, in vitro swelling, ex vivo mucoadhesion, in vitro drug release and in vivo x-ray imaging studies. Optimized pellets were sufficiently porous spheroids, free flowing, had smooth surfaces, had yields up to 75.45 ± 0.52% and had drug content up to 96.45 ± 0.19%. The average particle size of formulations MF2 and MF6 were 1.13 ± 0.41 mm and 1.22 ± 0.18 mm, respectively. Formulation MF6 exhibited strong adhesion, about 94.67%, to goat mucosal tissue, and the desired in vitro swelling, with a sustained drug release profile for 12 h and with retention in the upper small intestine of rabbits for 10 h. We conclude that hydroxy propyl methyl cellulose K200M and microcrystalline cellulose at a 2.80:1.00 w/w ratio could be an effective carrier for multiple unit controlled delivery of metformin hydrochloride.


Mahajan H.S.,R C Patel Institute Of Pharmaceutical Education And Research | Tatiya B.V.,R C Patel Institute Of Pharmaceutical Education And Research | Nerkar P.P.,R C Patel Institute Of Pharmaceutical Education And Research
Powder Technology | Year: 2012

The aim of this study was the production of ondansetron hydrochloride loaded polymeric microspheres for delivery via the nasal route with aim to avoid hepatic first-pass metabolism, and enhance residence time. The microspheres were prepared by the spray-drying technique using pectin as the polymer. The objective of this study was to examine extensively the influence of formulation and process variables on the characteristics of the microspheres prepared. The effects of various experimental parameters such as drug to polymer concentration and liquid feed flow rate on particle size and entrapment efficiency were evaluated by means of experimental factorial designs. A 3 2 full factorial design was employed in formulating the microspheres with polymer concentration (X 1) and liquid feed flow rate (X 2) as independent variables and particle size and entrapment efficiency were dependent variables. The results showed that the X 1X 2 interaction had effect on particle size where as X 2 alone effect on entrapment efficiency. The optimal microspheres were evaluated with respect to zeta potential study, drug release kinetic study, ex vivo permeation study, histological examination, stability study and in vivo study. Microspheres were characterized by differential scanning calorimetry, scanning electron microscopy and X-ray diffraction study. Scanning electron microscopy confirmed the smooth spherical surface of microspheres where as kinetic model revealed that drug release followed case II transport. The nasal delivery showed increased bioavailability as compared to oral delivery. In conclusion, the pectin containing microspheres of ondansetron hydrochloride with mucoadhesive property are suitable for nasal delivery. © 2012 Elsevier B.V.


Wagh V.D.,R C Patel Institute Of Pharmaceutical Education And Research
Advances in Pharmacological Sciences | Year: 2013

Propolis is a natural resinous mixture produced by honey bees from substances collected from parts of plants, buds, and exudates. Due to its waxy nature and mechanical properties, bees use propolis in the construction and repair of their hives for sealing openings and cracks and smoothing out the internal walls and as a protective barrier against external invaders like snakes, lizards, and so forth, or against weathering threats like wind and rain. Bees gather propolis from different plants, in the temperate climate zone mainly from poplar. Current antimicrobial applications of propolis include formulations for cold syndrome (upper respiratory tract infections, common cold, and flu-like infections), wound healing, treatment of burns, acne, herpes simplex and genitalis, and neurodermatitis. Worldwide propolis has a tremendous popularity, but in India the studies over propolis have just started, not extensively reported except few regions of India like Maharashtra, West Bengal, Tamil Nadu, Gujrat, and Madhya Pradesh. © 2013 Vijay D. Wagh.


Belgamwar V.S.,R C Patel Institute Of Pharmaceutical Education And Research | Surana S.J.,R C Patel Institute Of Pharmaceutical Education And Research
Chemical and Pharmaceutical Bulletin | Year: 2010

The aim of the present study was to prepare mucoadhesive multiparticulate system for oral drug delivery using ionic gelation technique. Microspheres of different mucoadhesive polymers including hydroxypropyl methylcellulose (HPMC) K15M and carbopol 971P were prepared. In this technique cross linking of sodium alginate with calcium chloride was done which retarded the release of drug from the mucoadhesive polymer. In the present work atenolol was used as model drug. Interaction studies performed using FT-IR spectroscopy revealed that there was no drug to polymer interactions. Multiparticulates so prepared were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 23-74%. Particle size of the multiparticulates as determined by the scanning electron microscopic analysis (SEM) studies was found to be between 561-831 μm. The prepared formulations also exhibited a good mucoadhesive strength which was determined in in vitro conditions through falling film technique. The multiparticulate so prepared also exhibited a good swelling index which confirmed the strong mucoadhesive property of the formulation. Atenolol release from the multiparticulate system was regulated and extended until 12 h and exhibited a non-Fickian anomalous transport from the swellable microspheres, as evident from the release rate exponent values which varied between 0.569-0.622. The stability studies performed on the optimized batch at 40 °C/75% RH for 90 d indicated no significant change in the physicochemical properties. In vivo radioimaging studies in rabbits showed the residence of mucoadhesive microspheres for 6-8 h in upper part of gastrointestinal tract (GIT). © 2010 Pharmaceutical Society of Japan.

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