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Pharmaceutics 2011, 3(4), 830-847; doi:10.3390/pharmaceutics3040830
Article

Formulation Optimization of Sustained-Release Ammonio Methacrylate Copolymer Microspheres. Effects of Log P and Concentration of Polar Cosolvents, and Role of the Drug/Copolymer Ratio

1,* , 2, 1, 1 and 1
Received: 29 June 2011; in revised form: 11 October 2011 / Accepted: 27 October 2011 / Published: 10 November 2011
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Abstract: The objectives of this work were the formulation optimization of the preparation process parameters and to evaluate spray-dried sustained-release microspheres using ammonio methacrylate copolymer (AMC) as a polymer matrix. The effects of log P and the concentrations of the cosolvents (acetone, methyl ethyl ketone and n-butyl acetate) and different drug/copolymer ratios as independent variables on the physicochemical parameters (the W1/O emulsion viscosity, the microsphere production yield, the average particle size, the encapsulation efficiency) and the cumulative in vitro drug release as dependent variables were studied. The optimization was carried out on the basis of the 33 factorial design study. The optimization process results showed that addition of polar cosolvents proved effective, linear relationships were observed between the independent and the dependent variables. The best conditions were achieved by microspheres prepared by using a low/medium cosolvent log P, cosolvent concentration of 25–50% v/v and a drug/copolymer ratio of 1:16. The microspheres ensured sustained release with Nernst and Baker-Lonsdale release profiles.
Keywords: microspheres; formulation optimization; cosolvents; drug/copolymer ratio; spray drying; factorial design study microspheres; formulation optimization; cosolvents; drug/copolymer ratio; spray drying; factorial design study
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.

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MDPI and ACS Style

Sipos, P.; Rajkó, R.; Pintye-Hódi, K.; Erős, I.; Szabó-Révész, P. Formulation Optimization of Sustained-Release Ammonio Methacrylate Copolymer Microspheres. Effects of Log P and Concentration of Polar Cosolvents, and Role of the Drug/Copolymer Ratio. Pharmaceutics 2011, 3, 830-847.

AMA Style

Sipos P, Rajkó R, Pintye-Hódi K, Erős I, Szabó-Révész P. Formulation Optimization of Sustained-Release Ammonio Methacrylate Copolymer Microspheres. Effects of Log P and Concentration of Polar Cosolvents, and Role of the Drug/Copolymer Ratio. Pharmaceutics. 2011; 3(4):830-847.

Chicago/Turabian Style

Sipos, Péter; Rajkó, Róbert; Pintye-Hódi, Klára; Erős, István; Szabó-Révész, Piroska. 2011. "Formulation Optimization of Sustained-Release Ammonio Methacrylate Copolymer Microspheres. Effects of Log P and Concentration of Polar Cosolvents, and Role of the Drug/Copolymer Ratio." Pharmaceutics 3, no. 4: 830-847.



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