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Photodynamic therapy has a great potential in the treatment of cervical cancer. The aim of this study was to develop bioadhesive pellets containing hexylaminolevulinate (HAL), a precursor of the photoactive substance PpIX, with a fast release for vaginal drug delivery. Pellets were produced by extrusion/spheronization, and Carbopol(®) 934 was used to obtain bioadhesive properties. A 2(2)-factorial design with center point investigating the HAL content (1 and 10%, w/w) and Carbopol(®) 934 content (1 and 8%, w/w) was set up. The most suitable formulations were mechanically stable and showed bioadhesive properties toward vaginal tissue. The drug load was released within 20 min in phosphate buffer pH 4 and 6.8 in the in vitro dissolution test. The stability of HAL in the pellet formulations varied, but the most stable formulation showed 96-97% HAL remaining in the formulation after 6-7 weeks of storage at accelerated temperature conditions (40 °C). The investigated formulations seem promising for vaginal delivery of HAL. Copyright © 2012 Elsevier B.V. All rights reserved.

Citation

Marianne Hiorth, Linda Liereng, Reidun Reinertsen, Ingunn Tho. Formulation of bioadhesive hexylaminolevulinate pellets intended for photodynamic therapy in the treatment of cervical cancer. International journal of pharmaceutics. 2013 Jan 30;441(1-2):544-54

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PMID: 23142497

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