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Molecules 2015, 20(8), 14684-14698; doi:10.3390/molecules200814684

Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability

1
Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, P.O. Box 146, Belgrade 11221, Serbia
2
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, P.O. Box 146, Belgrade 11221, Serbia
*
Author to whom correspondence should be addressed.
Academic Editors: Thomas Rades, Holger Grohganz and Korbinian Löbmann
Received: 9 June 2015 / Revised: 26 July 2015 / Accepted: 5 August 2015 / Published: 13 August 2015
(This article belongs to the Collection Poorly Soluble Drugs)
View Full-Text   |   Download PDF [1309 KB, uploaded 13 August 2015]   |  

Abstract

The majority of drugs have a low dissolution rate, which is a limiting step for their absorption. In this manuscript, solid dispersions (SD), solid self-microemulsifying drug delivery systems (S-SMEDDS) and solid self-nanoemulsifying drug delivery systems (S-SNEDDS) were evaluated as potential formulation strategies to increase the dissolution rate of carbamazepine. Influence of increased dissolution rate on permeability of carbamazepine was evaluated using PAMPA test. In S-SMEDDS and S-SNEDDS formulations, the ratio of liquid SMEDDS/SNEDDS and solid carrier (Neusilin® UFL2) was varied, and carbamazepine content was constant. In SD formulations, the ratio of carbamazepine and Neusilin® UFL2, was varied. Formulations that showed the best dissolution rate of carbamazepine (SD_1:6, SMEDDS_1:1, SNEDDS_1:6) were mutually compared, characterization of these formulations was performed by DSC, PXRD and FT-IR analyses, and a PAMPA test was done. All formulations have shown a significant increase in dissolution rate compared to pure carbamazepine and immediate-release carbamazepine tablets. Formulation S-SMEDDS_1:1 showed the fastest release rate and permeability of carbamazepine. DSC, PXRD and FT-IR analyses confirmed that in S-SMEDDS and S-SNEDDS carbamazepine remained in polymorph form III, and that it was converted to an amorphous state in SD formulations. All formulations showed increased permeability of carbamazepine, compared to pure carbamazepine. View Full-Text
Keywords: carbamazepine; dissolution rate; PAMPA test; solid dispersions; S-SMEDDS; S-SNEDDS; characterization carbamazepine; dissolution rate; PAMPA test; solid dispersions; S-SMEDDS; S-SNEDDS; characterization
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Krstić, M.; Popović, M.; Dobričić, V.; Ibrić, S. Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability. Molecules 2015, 20, 14684-14698.

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