Formulation of benzoporphyrin derivatives in Pluronics.
This study investigates the potential of Pluronics for the formulation of tetrapyrrole-based photosensitizers, with a particular focus on B-ring benzoporphyrin derivatives. The B-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.
Chowdhary
Rubinah K
RK
Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia, Canada.
Chansarkar
Namrata
N
Sharif
Isha
I
Hioka
Noboru
N
Dolphin
David
D
D016503:Drug Delivery Systems; D004355:Drug Stability; D010777:Photochemistry; D017319:Photosensitizing Agents / Q000737:chemistry*; D020442:Poloxamer; D011166:Porphyrins / Q000737:chemistry*
D017319:Photosensitizing Agents; D011166:Porphyrins; D020442:Poloxamer