Abiraterone acetate (AbA) is a progesterone derivative indicated for the treatment of metastatic prostate cancer. This BCS (Biopharmaceutics Classification System) Class IV molecule has an extremely poor oral bioavailability (<10 %), notably due to its very low water solubility and intestinal permeability. Among the few existing galenic strategies to improve AbA's oral bioavailability, lipid nanoparticles such as Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) are relevant nanovectors.
View Article and Find Full Text PDFThis unique work is targeted to achieve three main goals: i) to enhance the aqueous solubility of three specifically selected hydrophobic active agents, ii) to prepare such polymeric biodegradable microparticles which can encapsulate actives-cyclodextrin complexes and iii) to functionalize a polyamide base textile with active loaded microparticles and active-cyclodextrin loaded microparticles. To achieve this objective, biodegradable cationic microparticles were prepared via double emulsion solvent evaporation process and were loaded with hydroxypropyl-beta-cyclodextrin based complexes of Indomethacin, α-tocopheroland Lauryl Isoquinolinium Bromide during the formulation process. Inclusion complex based particles were evaluated for their morphology, size distribution, zeta potential, skin penetration aptitude and adsorption onto a selected textile.
View Article and Find Full Text PDFIn this work, the formation and stability of amorphous solid dispersions (SDs) as orodispersible films (ODF) were investigated using tetrabenazine (TBZ) as a poorly water soluble drug. The influence of polymer nature and pH-modifier incorporation to form and maintain SDs was investigated. TBZ-loaded ODF were formulated using 4 different polymers (HPMC, PVP, Pullulan, and HEC).
View Article and Find Full Text PDFThe aim of present work is to investigate systematic study of the preparation of biodegradable particles via double emulsion solvent evaporation technique. The used formation is based on cationic ammonium methacrylate copolymer Eudragit® RS 100, without the use of any stabilizer. The effect of process parameters like ultra turrax® stirring speed and stirring time, ultrasonication time, polymer amount, and volume of outer aqueous phases on the colloidal properties of particles was investigated.
View Article and Find Full Text PDFBlock copolymer nanoparticles often referred to as "block copolymer micelles" have been assessed as carriers for skin delivery of hydrophobic drugs. Such carriers are based on organic biocompatible and biodegradable materials loaded with hydrophobic drugs: poly(lactide)-block-poly(ethylene glycol) copolymer (PLA-b-PEG) nanoparticles that have a solid hydrophobic core made of glassy poly(d,l-lactide), and poly(caprolactone)-block-poly(ethylene glycol) copolymer (PCL-b-PEG) nanoparticles having a liquid core of polycaprolactone. In vitro skin absorption of all-trans retinol showed a large accumulation of retinol in stratum corneum from both block copolymer nanoparticles, higher by a factor 20 than Polysorbate 80 surfactant micelles and by a factor 80 than oil solution.
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