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1 March 2003 Formulation of Benzoporphyrin Derivatives in Pluronics
Rubinah K. Chowdhary, Namrata Chansarkar, Isha Sharif, Noboru Hioka, David Dolphin
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Abstract

This study investigates the potential of Pluronics for the formulation of tetrapyrrole-based photosensitizers, with a particular focus on B-ring benzoporphyrin derivatives. TheB-ring derivatives have a high tendency to aggregate in aqueous solutions, and this poses a significant formulation problem. Pluronics are ABA-type triblock copolymers composed of a central hydrophobic polypropylene oxide section with two hydrophilic polyethylene oxide sections of equal length at either end. Out of a range of different commercially available block copolymers studied, it was found that the longer the hydrophobic block, the better the stabilization of tetrapyrrolic drugs in monomeric form in aqueous suspensions. Of these the best performance was observed in the micelle-forming Pluronic P123. Micelle size determination by laser light scattering confirmed that particle size in stable Pluronic formulations was around 20 nm. Pluronics such as L122 formed emulsions spontaneously without the need for emulsion stabilizers; emulsions were highly stable at ambient temperatures over several days and also highly effective as potential drug delivery agents.

Rubinah K. Chowdhary, Namrata Chansarkar, Isha Sharif, Noboru Hioka, and David Dolphin "Formulation of Benzoporphyrin Derivatives in Pluronics," Photochemistry and Photobiology 77(3), 299-303, (1 March 2003). https://doi.org/10.1562/0031-8655(2003)077<0299:FOBDIP>2.0.CO;2
Received: 6 June 2002; Accepted: 1 November 2002; Published: 1 March 2003
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