Institute of Pharmaceutical Education and Research IPER

Wardha, India

Institute of Pharmaceutical Education and Research IPER

Wardha, India
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Khan S.,Institute of Pharmaceutical Education and Research IPER | Patil K.,Institute of Pharmaceutical Education and Research IPER | Bobade N.,Institute of Pharmaceutical Education and Research IPER | Yeole P.,Institute of Pharmaceutical Education and Research IPER | Gaikwad R.,Nuclear Medicine Center
Journal of Drug Targeting | Year: 2010

Mucoadhesive temperature-mediated in situ gel formulations using chitosan and hydroxyl propyl methyl cellulose were used to enhance intranasal (i.n.) delivery of the dopamine D2 agonist ropinirole to the brain. Formulations were tested for gelation time, thermosensitivity, mucoadhesion, in vitro release and permeation, in vitro cytotoxicity, nasal clearance, in vivo bioavailability and brain uptake. In vivo bioavailability and brain uptake of ropinirole were assessed in albino rats following intranasal administration of 99mTc-ropinirole in situ gel, intranasal ropinirole solution and intravenous (i.v.) ropinirole solution. Radiolabeled ropinirole uptake was calculated as a fraction of administered dose. The absolute bioavailabilty of ropinirole from the temperature-mediated in situ gelling nasal formulation was 82%. The AUC 0-480 min in brain after nasal administration of ropinirole in situ gel was 8.5 times (869±250% · min/g versus 102±20% · min/g) that obtained following i.v. administration, this value was also considerably higher (869±250% · min/g versus 281± 52%·min/g) than that achieved with intranasal ropinirole solution. High brain direct drug transport percentage (DTP; 90.36%) and drug targeting index (DTI) > 1 confirms direct nose to brain transport of the intranasal in situ gel formulation of ropinirole. © 2010 Informa UK Ltd.


Takarkhede K.,Institute of Pharmaceutical Education and Research IPER | Singhavi D.J.,Institute of Pharmaceutical Education and Research IPER | Khan S.,Institute of Pharmaceutical Education and Research IPER | Yeole P.,Institute of Pharmaceutical Education and Research IPER
Thai Journal of Pharmaceutical Sciences | Year: 2012

Furosemide is poorly soluble in acidic pH and absorbed from the upper part of the GI tract. We, therefore, aimed to develop a sustained release gastroretentive beads containing furosemide inclusion complex. The different formulations of floating beads were prepared by using swellable mucoadhesive polymers (sodium alginate and hydroxypropyl methylcellulose) and sodium bicarbonate as an effervescent agent. The prepared beads were coated with different concentration of chitosan HCl solution and evaluated for encapsulation efficiency, loading efficiency, mucoadhesion, swelling, floating properties, particle size, in vitro release characteristic and surface morphology. The effect of different level of furosemide inclusion complex and chitosan HCl coating on beads performance was studied. The formulation (F4) coated with 1% w/v chitosan coating level gave 98 ± 1% floating efficiency, 93 ± 3% mucoadhesion, 85.81 ± 3.24% swelling index and 94.04 ± 2.45% release of furosemide at the end of 12 h. In vitro release data for optimized formulation demonstrated non fickian mechanism. An optimized formulation was subjected to stability studies for six months which showed stability with regards to release pattern. The floating beads proved to be a promising gastroretentive drug delivery system for furosemide.


Khade K.V.,Institute of Pharmaceutical Education and Research IPER | Dubey H.,Institute of Pharmaceutical Education and Research IPER | Tenpe C.R.,Institute of Pharmaceutical Education and Research IPER | Yeole P.G.,Institute of Pharmaceutical Education and Research IPER | Patole A.M.,Institute of Pharmaceutical Education and Research IPER
Pharmacologyonline | Year: 2011

The present study was designed to determine the anticancer activity of the ethanolic extract of leaves of Agave americana L. (Agavaceae) using three reported methods. For brine shrimp lethality bioassay ten nauplii were placed in test tube filled with 5 ml total volume of artificial sea water and different concentrations (100, 500, 1000, 2000, 5000 μg/ml) of ethanolic extract of Agave americana leaves in a set of test tubes per dose. After 24 hours, live nauplii were counted and LC50 value was estimated. In Allium cepa root meristem model, onion bulbs were suspended inside 100 ml beakers at different concentration (1 mg/ml and 10 mg/ml) of extract. The percentage root growth inhibition after treating with ethanolic extract at 48 and 96 hrs was determined. MTT assay have been utilised to measure the antitumor activity of ethanolic extract of A. americana leaves by using PA-1 human cell line of ovarian teratocarcinoma. Brine shrimp lethality bioassay (LC50= 923.10μg/ml), Allium cepa root meristem model and MTT assay (IC50 =0.01μg/ml) showed potent cytotoxic and anticancer activity of ethanolic extract of A. americana leaves. The ethanolic extract of A. americana leaves has a cytotoxic and antitumor activity. Therefore, this plant has potential to be utilized for the development of novel anticancer drug leads.


Ravi R.G.,Institute of Pharmaceutical Education and Research IPER | Harikesh D.,Institute of Pharmaceutical Education and Research IPER | Chandrasekhar T.R.,Institute of Pharmaceutical Education and Research IPER | Pramod Y.G.,Institute of Pharmaceutical Education and Research IPER | Angad P.M.,Institute of Pharmaceutical Education and Research IPER
International Journal of Drug Development and Research | Year: 2011

The present study deals with the cytotoxic activity of the ethanolic root extract of C. gigantea Linn. The different concentrations of ethanolic extract of the roots of C. gigantea Linn were used for cytotoxic activity by Brine shrimp lethality bioassay (BSLB) and Allium cepa root meristem (ACRM) models. In BSLB, LC 50 value was found to be 62.12μg/ml while LC 50 value of cyclophosphamide was found to be 41.54μg/ml. In ACRM model, incubation of onion bulbs in different concentrations of extract produced a growth retarding effect that was associated with a decrease in the root number. ACRM growth inhibition was highest with significance of (p<0.01) at the 10 mg/ml concentration after 48 hrs incubation for ethanolic root extract. Extract produced dose and time dependent growth inhibition. The ethanolic root extract of C. gigantea exhibits potent cytotoxic property comparable to that of standard drug. Therefore, this might be utilized for the development of novel anticancer drug leads. © 2010 IJDDR.


Shaikh A.,Institute of Pharmaceutical Education and Research IPER | Yeole P.G.,Institute of Pharmaceutical Education and Research IPER | Iyer D.,Institute of Pharmaceutical Education and Research IPER
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2013

The solubility behaviour of drug is one of most challenging aspect in formulation development. Thus a greater understanding of dissolution & absorption behaviour of drug with low aqueous solubility is required to successfully formulate them into more soluble and hence bioavailable drug product. The current investigation includes formulating solid dispersions of Tinidazole, an antiprotozoal and antiamoebic drug which is characterized by poor solubility and rapid absorption (BCS-2). Thus an attempt was made to prepare stable solid dispersion by improving the solubility and dissolution rate of tinidazole using a mixture of polymers viz: hydroxypropylmethyl cellulose (HPMC), Polaxomer-F-188 (POL), Polyvinyl pyrrolidone (PVP), Polyethylene glycol (PEG) and polymeric surfactants in different proportions as carrier. Solid dispersions of tinidazole were prepared by spray drying technique, melting technique and as physical mixture to conduct a comparative evaluation of the methods that could yield the most stable formulation and then were evaluated for number of analytical parameters. Solid dispersions containing Drug: PEG 6000: Poloxamer 188 as carrier in 1:0.3:0.2 ratios by melting method showed the best result. POL and PEG combination revealed a synergistic effect, on solubility, dissolution and stability of crystalline drug and both crystallization inhibitor (PEG) and wetting agent (poloxamer) in solid dispersion can improve solubility and release profile of tinidazole. The study demonstrates high potential of Melting method for obtaining large surface area and amorphicity of drug using hydrophilic carrier. The solid dispersions were compressed into Fast Dissolving Tablets by incorporating appropriate superdisintegrants.


PubMed | Institute of Pharmaceutical Education and Research IPER
Type: Comparative Study | Journal: Journal of drug targeting | Year: 2010

Mucoadhesive temperature-mediated in situ gel formulations using chitosan and hydroxyl propyl methyl cellulose were used to enhance intranasal (i.n.) delivery of the dopamine D2 agonist ropinirole to the brain. Formulations were tested for gelation time, thermosensitivity, mucoadhesion, in vitro release and permeation, in vitro cytotoxicity, nasal clearance, in vivo bioavailability and brain uptake. In vivo bioavailability and brain uptake of ropinirole were assessed in albino rats following intranasal administration of 99mTc-ropinirole in situ gel, intranasal ropinirole solution and intravenous (i.v.) ropinirole solution. Radiolabeled ropinirole uptake was calculated as a fraction of administered dose. The absolute bioavailabilty of ropinirole from the temperature-mediated in situ gelling nasal formulation was 82%. The AUC (0-480 min) in brain after nasal administration of ropinirole in situ gel was 8.5 times (869 +/- 250% x min/g versus 102 +/- 20% x min/g) that obtained following i.v. administration, this value was also considerably higher (869 +/- 250% x min/g versus 281 +/- 52% x min/g) than that achieved with intranasal ropinirole solution. High brain direct drug transport percentage (DTP; 90.36%) and drug targeting index (DTI) > 1 confirms direct nose to brain transport of the intranasal in situ gel formulation of ropinirole.

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