Microencapsulation of hydroxyzine HCl by thermal phase separation: in vitro release enhancement and in vivo pharmacodynamic evaluation

Citation:
Latif, R., C. M. Zaki, and I. I. Soliman, "Microencapsulation of hydroxyzine HCl by thermal phase separation: in vitro release enhancement and in vivo pharmacodynamic evaluation", Pharmaceutical Development and Technolgy, vol. 12, issue 3, pp. 989-1002, 2013.

Abstract:

Hydroxyzine HCl is used in oral formulations for the treatment of urticaria and atopic
dermatitis. Dizziness, blurred vision, and anticholinergic responses, represent the most common side
effects. It has been shown that controlled release of the drug from a delivery system to the skin could
reduce the side effects while reducing percutaneous absorption. Therefore, the aim of the present study
was to produce an effective drug-loaded dosage form that is able to control the release of hydroxyzine
hydrochloride into the skin. The Microsponge Delivery System is a unique technology for the controlled
release of topical agents, and it consists of porous polymeric microspheres, typically 10–50 μm in
diameter, loaded with active agents. Eudragit RS-100 microsponges of the drug were prepared by the oil
in an oil emulsion solvent diffusion method using acetone as dispersing solvent and liquid paraffin as the
continuous medium. Magnesium stearate was added to the dispersed phase to prevent flocculation of
Eudragit RS-100 microsponges. Pore inducers such as sucrose and pregelatinized starch were used to
enhance the rate of drug release. Microsponges of nearly 98% encapsulation efficiency and 60–70%
porosity were produced. The pharmacodynamic effect of the chosen preparation was tested on the
shaved back of histamine-sensitized rabbits. Histopathological studies were driven for the detection of
the healing of inflamed tissues.

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