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In Vitro and In Vivo Evaluation of Hydroxyzine Hydrochloride Microsponges for Topical Delivery

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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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Authors and Affiliations

  1. Faculty of Pharmacy, Cairo University, Kasr Einy, Egypt

    Christianne Mounir Zaki Rizkalla & Randa latif Aziz

  2. Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia

    Iman Ibrahim Soliman

Authors
  1. Christianne Mounir Zaki Rizkalla
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  2. Randa latif Aziz
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  3. Iman Ibrahim Soliman
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Correspondence to Christianne Mounir Zaki Rizkalla.

Additional information

The protocol of the present work was approved by the Experiments and Advanced Pharmaceutical Research Unit (EAPRU), Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Any experiments involving the use of animals were conducted in accordance with the principles of Laboratory Animal Care and were approved by the institutional ethics committee.

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Zaki Rizkalla, C.M., latif Aziz, R. & Soliman, I.I. In Vitro and In Vivo Evaluation of Hydroxyzine Hydrochloride Microsponges for Topical Delivery. AAPS PharmSciTech 12, 989–1001 (2011). https://doi.org/10.1208/s12249-011-9663-5

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