Title |
THE CHALLENGES OF OPHTHALMIC DRUG DELIVERY: A REVIEW |
| Int J Drug Discov Vol:3 Iss:1 (2011-07-21) : 56-62 |
Authors |
HEMING T., SINGH V., AHMAD R. |
Published on |
21 Jul 2011 Pages : 56-62 Article Id : BIA0000180 Views : 1103 Downloads : 974 |
DOI | http://dx.doi.org/10.9735/0975-4423.3.1.56-62 |
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Abstract |
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During the past decades, researchers involved in the development of ophthalmic pharmaceuticals have
understood that ophthalmic drug delivery is a challenging subject for optimization. Normal vision is dependent
upon the optimal functioning of ocular barriers and intact membranes that function to selectively regulate the
environment of ocular tissues. Novel pharmacotherapeutic modalities have aimed to overcome the biological
barriers which can impede efficient ocular drug delivery. To explore the impact of ocular barriers on research
related to ophthalmic drug delivery and targeting, herein we provide a review of the literature of work carried out
on the biological constraints and new approaches to ophthalmic drug delivery.
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Title |
A LINEAR QSAR AND DOCKING APPROACH TO MODEL INHIBITORY ACTIVITY OF 2-ARYLBENZOXAZOLE DERIVATIVES AS CHOLESTERYL ESTER TRANSFER PROTEIN (CETP) INHIBITORS |
| Int J Drug Discov Vol:3 Iss:1 (2011-07-21) : 63-73 |
Authors |
MUKESH YADAV, ANURAJ NAYARISSERI, SHOBHA JOSHI, ANKITA GUPTA, PURVA HOLKAR, ASHISH RAJPUT |
Published on |
21 Jul 2011 Pages : 63-73 Article Id : BIA0000181 Views : 1035 Downloads : 1026 |
DOI | http://dx.doi.org/10.9735/0975-4423.3.1.63-73 |
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QSAR studies of thirty 2-arylbenzoxazole derivatives are carried out to probe their inhibitory activity
against Cholesteryl Ester Transfer Protein (CETP). QSAR models have been obtained using multiple linear
regression (MLR) analysis after manifestation of forward selection algorithm to cull significant descriptors out of
descriptor’s pool. QSAR models are elected with adherent set of statistical parameters with R2=0.9431 and
R2=0.9069. Validation of modeling includes method of Y-Scrambling and in addition to this, some other methods
of validation. Moreover, QSAR approach of 2-arylbenzoxazoles are also attempted, supported and validated by
flexible docking studies as well. The search strategies include evolutionary algorithm and edited form of Gehlhaar
PLP scoring function. The same set of thirty candidates from 2-arylbenzoxazole derivatives is processed in
molecular docking and their docking scores are found in agreement with QSAR studies reported. Remarkable
CETP inhibitory activity is exhibited by a 2-arylbenzoxazole derivatives molecule 29C with most comprehensive
set of interactions with rerank scores -102.167 and RMSD values 1.104. Hydrogen bond interactions along with
hydrophobic and electrostatic interactions are mapped to confirm their potencies.
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Title |
AN INVESTIGATION ON CYTOTOXIC AND ANTIOXIDANT PROPERTIES OF CLITORIA TERNATEA L. |
| Int J Drug Discov Vol:3 Iss:1 (2011-07-21) : 74-77 |
Authors |
VIDHYA RAMASWAMY, NEETHU VARGHESE, ANCY SIMON |
Published on |
21 Jul 2011 Pages : 74-77 Article Id : BIA0000182 Views : 1117 Downloads : 1028 |
DOI | http://dx.doi.org/10.9735/0975-4423.3.1.74-77 |
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Abstract |
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The ethanolic extract of Clitoria ternatea L. was evaluated for its in vitro cytotoxic and antioxidant activities. The extract showed potent cytotoxic activity in trypan blue dye exclusion method using DLA cell lines with EC50 value of 305μg/ml and exhibited a dose dependent decrease in cell count for all the concentrations tested. The antioxidant activity was evaluated by DPPH free radical method. The extract exhibited potent antioxidant activity with an EC50 of 36.5μg/ml.
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