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Original Research Article | OPEN ACCESS

Development and Evaluation of Praziquantel Solid Dispersions in Sodium Starch Glycolate

Marco V Chaud1 , Andréa C Lima2, Marta MDC Vila1, Maria O Paganelli3, Fábio C Paula4, Liliane N Pedreiro4, Maria PD Gremião5

1Laboratory for Development and Evaluation of Bioactive Substances, Sorocaba University (UNISO), Sorocaba, SP; 2Piracicaba Methodist University, Piracicaba, SP; 3Campinas University, UNICAMP. Campinas, SP; 4Ribeirão Preto University (UNAERP), Ribeirão Preto-SP; 5São Paulo State University, UNESP. Araraquara, SP, Brazil.

For correspondence:-  Marco Chaud   Email: marco.chaud@prof.uniso.br   Tel:+551521017104

Received: 29 May 2012        Accepted: 27 January 2013        Published: 24 April 2013

Citation: Chaud MV, Lima AC, Vila MM, Paganelli MO, Paula FC, Pedreiro LN, et al. Development and Evaluation of Praziquantel Solid Dispersions in Sodium Starch Glycolate. Trop J Pharm Res 2013; 12(2):163-168 doi: 10.4314/tjpr.v12i2.5

© 2013 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..

Abstract

Purpose: To develop and characterize solid dispersions of praziquantel (PZQ) with sodium starch glycolate (SSG) for enhanced drug solubility.
Methods: PZQ solid dispersion (SD) was prepared using co-precipitation method by solvent evaporation. The ratios of PZQ to SSG were 2:1, 1:1, 1:2, 1:3 (w/w). PZQ solubility was evaluated in purified water, and PZQ dissolution test was carried out in 0.1N HCl. Structural characterization of the dispersions was accomplished by x-ray diffraction (XRD) and infrared spectroscopy (FTIR) while the external morphology of the SDs, SSG and PZQ were studied by scanning electron microscopy (SEM). Mucoadhesion properties of the SD (1:3) and SSG, on mucin disks were examined using texture profile analysis.
Results: The highest solubility was obtained with 1:3 solid dispersion, with PZQ solubility of 97.31 %, which is 3.65-fold greater than the solubility of pure PZQ and physical misture (PM, 1:3). XRD results indicate a reduction in PZQ crystallinity while infrared spectra showed that the functional groups of PZQ and SSG were preserved. SEM showed that the physical structure of PZQ was modified from crystalline to amorphous. The amount of PZQ in PM and SD (1:3) that dissolved in 60 min was 70 and 88 %, respectively, and these values increased to 76 and 96 %, respectively. The solid dispersion reduced the mucoadhesive property of the glycolate.
Conclusion: Solid dispersion formulation using SSG is a good alternative approach for increasing the dissolution rate of PZQ.

Keywords: Praziquantel, Drug bioavailability, Schistosomiasis, Solid dispersion, Co-precipitation, Sodium starch glycolate

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Thompson Reuters (ISI): 0.6 (2023)
H-5 index (Google Scholar): 49 (2023)

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