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Titlar
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    Novel Block Copolymer Self-Assembled Micelles as Nanocarriers for Drug Delivery. Preparation, Characterization and In Vitro Evaluation

  • Mísellur sem myndast af sjálfsdáðum úr nýstárlegum bjálka-samfjölliðum sem nanó-flutningskerfi fyrir lyf. Undirbúningur, eiginleikar og in vitro prófanir

Útdráttur

The continuous search for new drug delivery systems is driven by the ardour to maximize therapeutic activity while minimizing negative side effects. Particularly, much attention is now being paid to amphiphilic polymeric micelles as nanocarriers for drug delivery systems. Block copolymer micelles as drug carriers are able to provide highly desirable advantages including increased solubilization of poorly soluble drugs. Poor aqueous solubility is a big obstacle in drug development. It poses such a serious problem that some pharmaceutical companies decide to exclude poorly soluble compounds very early in their screening process regardless of how active these compounds are. It has repeatedly been shown that polymeric micelles can increase the solubility of poorly aqueous soluble drugs. Compared to other drug carriers, micelles can be obtained in an easy and reproducible manner on a large scale. The nano-size of the polymeric micelles not only makes them ideal drug delivery carriers as they escape from renal exclusion but also enhances their vascular permeability. The aim of this research project was to explore the solubilizing potential of a novel block copolymer, Boc-(Leu-Leu-Ala-Lac)5-Leu-Phe-O-PEG4000-OH, also named DP7, through micellization of poorly soluble drugs in order to improve their bioavailability. Another objective was to characterize the micelles and to evaluate if fatty acids, such as stearic acid, could improve the efficacy of DP7 micelles. The results show that DP7 self-aggregate and form nano-size micelles which greatly enhance the solubility of fenofibrate, which is a very poorly soluble drug in aqueous solutions. It was also observed that stearic acid enhanced the drug entrapment efficiency of the micelles but the inclusion of stearic acid did not result in slow drug diffusion from the micelles in in vitro studies. Future studies will determine the behaviour of DP7 micelles in vivo and their feasibility in drug targeting.

Birting
11.5.2009


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