A new pH-sensitive micelle delivery system based on TAT cell penetrating peptide and biodegradable sulfonamide grafted disulfide polymer is presented. The system consists of two components: (1) A polymeric micelle made of Poly(L-lactic acid)-b-poly(ethylene glycol) (PLLA-b-PEG) conjugated to TAT (TAT-micelle), (2) A pH-sensitive diblock copolymer (poly(L-cystine bisamide-g-sulfadiazine))-b-PEG (PCBS-b-PEG). The anionic PCBS complexed with cationic TAT of TAT-micelles forms the final carrier. PCBS showed rapid degradation in the presence of cysteine. The TAT-micelles showed increase in particle size between pH 8.0 and 7.0 upon mixing with PCBS-b-PEG indicating complexation. As the pH was further decreased (pH 6.8 to 6.0) two populations were observed, one of normal TAT-micelles and the other of aggregated PCBS-b-PEG. Flow cytometry showed significantly higher uptake of TAT-micelles at pH 6.6 indicating deshielding compared to pH 7.4. The anticancer drug doxorubicin (DOX) was encapsulated into the TAT-micelles, and the in vitro cytotoxicity at different pHs was evaluated. The system was able to distinguish pHs 7.2 and 7.0 in terms of cytotoxicity.
A series of polymeric emulsifiers was polymerized with 2-ethylhexyl acrylate, butyl acrylate, and acrylic acid. The polymeric emulsifiers were used to make emulsion copolymers of 2-ethylhexyl acrylate, butyl acrylate, and acrylic acid. The average particle size of the synthesized emulsions was around 145 nm and the size distribution was very narrow. Also, the emulsions showed good freeze-thaw stability and adhesion properties. The peel strength and holding power of the emulsions were investigated by changing the composition and molecular weight of the polymeric emulsifier. The results show that the peel strength exhibits a maximum at particular molecular weight and acrylic acid content of the polymeric emulsifier, while the holding power increases with molecular weight.
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