Prediction of drug solubility in amphiphilic di-block copolymer micelles: the role of polymer-drug compatibility
The goal of the current study was to assess the value of predictive computational approaches for estimating drug solubility in hydrated micelles formed from di-block copolymers of polyethylene glycol (PEG) and random copolyesters of ɛ-caprolactone (CL) and trimethylene carbonate
(TMC) using drug-polymer compatibility as assessed through the Flory-Huggins interaction parameter (χ). In order to accomplish this, the compatibility of several well-known model drugs (associated with the four biopharmaceutics classification system (BCS) classes) was assessed with both
segments of the amphiphilic di-block copolymer PEG-b-P(CL-co-TMC). Compatibilities were estimated based on the Hansen modification of the Hildebrand approach using Molecular Modeling Pro software. Experimental solubilities for model drugs were determined using a shake-flask technique at various
polymer concentrations. The solubilities of 8 compounds in 10% w/v micelle solutions were in relatively good agreement with the predicted drug-polymer compatibility. In addition, the approach allows for the selection of a suitable di-block copolymer for optimal solubilization of a specific
drug. Furosemide was assessed as a model with results suggesting that it can be best entrapped in a di-block copolyester containing a relatively high CL content. The data suggests that prediction of drug solubilization of block copolymer-based micelles may be facilitated by assessing the compatibility
of the drug for the component polymeric domains.
Document Type: Research Article
Affiliations: 1: Johnson & Johnson Pharmaceutical Research and Development, Janssen Pharmaceutica, Pharmaceutical Sciences, Beerse, Belgium 2: Current Address: Cordis Corporation, Waren, NJ, USA 3: Department of Pharmaceutical Technology, Université Catholique de Louvain, Brussels, Belgium 4: Johnson & Johnson Pharmaceutical Research and Development, Janssen Pharmaceutica, Pharmaceutical Sciences, Turnhousteweg 30, Beerse, 2340, Belgium, Email: [email protected]
Publication date: 01 July 2007
- Pharmazie is a leading journal in the field of pharmaceutical sciences. As a peer-reviewed scientific journal, Pharmazie is regularly indexed in the relevant databases like Web of science, Journal Citation Reports and many others. The journal is open for submissions from the whole spectrum of pharnaceutical sciences including Pharmaceutical Chemistry, Experimental and Clinical Pharmacology, Drug Analysis, Pharmaceutics, Pharmaceutical Biology, Clinical Pharmacy etc.
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