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Pluronic lecithin organogel (PLO) of diltiazem hydrochloride: effect of solvents/penetration enhancers on ex vivo permeation

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Abstract

In the present study, pluronic lecithin organogel (PLO) of diltiazem hydrochloride (DZH) was developed by taking different ratios of organic phase to aqueous phase (1:3, 1:4, and 1:5) with varying concentration of soya lecithin (20, 30, and 40 % w/w) in organic phase (isopropyl myristate, IPM) and pluronic (20, 25, and 30 % w/w) in aqueous phase, respectively, and characterized for in vitro parameters and ex vivo permeation study. The results of in vitro parameters were found to be within permissible limit and all the PLOs were physically stable at refrigeration and ambient temperature. The influence of phase ratio and different concentrations of soya lecithin on DZH release from the PLOs was found to be significant (p < 0.05), whereas the influences of different concentrations of pluronic were insignificant. The effect of different solvents/penetration enhancers viz. IPM, propylene glycol (PG), dimethyl sulphoxide (DMSO), and d-limonene, in combination and alone, on the permeation of DZH across the dorsal skin of rat was studied. Among all, formulation containing IPM (PLO6) exhibited highest flux of 147.317 μg/cm2/h. Furthermore, histopathology section of treated skin sample illustrated that lipid bilayer disruption was the mechanism for the DZH permeation. The above results indicated that PLO6 may serve as a promising alternative delivery system for DZH in the effective treatment of hypertension.

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Acknowledgments

The authors acknowledge Dr. Durga Prasad, Professor of Histopathology, Department of Histology, NRI medical college for performing the histology studies.

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Authors and Affiliations

  1. Institute of Pharmacy, GITAM University, Gandhi Nagar Campus, Rushikunda, Visakhapatnam, 530045, Andhra Pradesh, India

    Rabinarayan Parhi

  2. Institute of Pharmacy and Technology, Salipur, 754202, Cuttack, Odisha, India

    Podilam Suresh

  3. P.G. Department of Zoology, Berhampur University, Berhampur, 760007, Odisha, India

    Subasini Pattnaik

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  1. Rabinarayan Parhi
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  3. Subasini Pattnaik
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Correspondence to Rabinarayan Parhi.

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Parhi, R., Suresh, P. & Pattnaik, S. Pluronic lecithin organogel (PLO) of diltiazem hydrochloride: effect of solvents/penetration enhancers on ex vivo permeation. Drug Deliv. and Transl. Res. 6, 243–253 (2016). https://doi.org/10.1007/s13346-015-0276-5

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