Copolymer Composition and Nanoparticle Configuration Enhance in vitro Drug Release Behavior of Poorly Water-soluble Progesterone for Oral Formulations
| Autor: | Upulitha Eranka Illangakoon, Mohan Edirisinghe, Christopher Thrasivoulou, Maryam Parhizkar, A. H. Harker, Rui Zhang, Yue Zhang, C. J. Luo |
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| Rok vydání: | 2020 |
| Předmět: |
Pharmaceutical Science
Nanoparticle 02 engineering and technology 01 natural sciences Crystallinity chemistry.chemical_compound Drug Delivery Systems poly Polylactic Acid-Polyglycolic Acid Copolymer X-Ray Diffraction International Journal of Nanomedicine Spectroscopy Fourier Transform Infrared Drug Discovery Copolymer poorly water-soluble drugs Original Research Drug Carriers Chemistry PLGA General Medicine lactide-co-glycolide oral formulations 021001 nanoscience & nanotechnology Drug delivery 0210 nano-technology coaxial electrospray Drug Compounding Biophysics Biological Availability Bioengineering progesterone 010402 general chemistry Biomaterials Particle Size Fourier transform infrared spectroscopy copolymer Organic Chemistry Water core-shell nanoparticles 0104 chemical sciences Bioavailability Drug Liberation Solubility Chemical engineering drug delivery Microscopy Electron Scanning Nanoparticles Pharmaceutics Spectrophotometry Ultraviolet bioavailability |
| Zdroj: | International Journal of Nanomedicine |
| ISSN: | 1178-2013 |
| DOI: | 10.2147/ijn.s257353 |
| Popis: | Yue Zhang,1 Rui Zhang,1 Upulitha Eranka Illangakoon,1,2 Anthony Henry Harker,3 Christopher Thrasivoulou,4 Maryam Parhizkar,1,2 Mohan Edirisinghe,1 CJ Luo1 1Department of Mechanical Engineering, University College London, London WC1E 7JE, UK; 2UCL School of Pharmacy, University College London, London WC1N 1AX, UK; 3Department of Physics & Astronomy, University College London, London WC1E 6BT, UK; 4Cell & Developmental Biology, Division of Biosciences, University College London, London WC1E 6BT, UKCorrespondence: CJ Luo Tel +44 20 7679 3942Email chaojie.luo@ucl.ac.ukHypothesis: Developing oral formulations to enable effective release of poorly water-soluble drugs like progesterone is a major challenge in pharmaceutics. Coaxial electrospray can generate drug-loaded nanoparticles of strategic compositions and configurations to enhance physiological dissolution and bioavailability of poorly water-soluble drug progesterone.Experiments: Six formulations comprising nanoparticles encapsulating progesterone in different poly(lactide-co-glycolide) (PLGA) matrix configurations and compositions were fabricated and characterized in terms of morphology, molecular crystallinity, drug encapsulation efficiency and release behavior.Findings: A protocol of fabrication conditions to achieve 100% drug encapsulation efficiency in nanoparticles was developed. Scanning electron microscopy shows smooth and spherical morphology of 472.1± 54.8 to 588.0± 92.1 nm in diameter. Multiphoton Airyscan super-resolution confocal microscopy revealed core-shell nanoparticle configuration. Fourier transform infrared spectroscopy confirmed presence of PLGA and progesterone in all formulations. Diffractometry indicated amorphous state of the encapsulated drug. UV-vis spectroscopy showed drug release increased with hydrophilic copolymer glycolide ratio while core-shell formulations with progesterone co-dissolved in PLGA core exhibited enhanced release over five hours at 79.9± 1.4% and 70.7± 3.5% for LA:GA 50:50 and 75:25 in comparison with pure progesterone without polymer matrix in the core at 67.0± 1.7% and 57.5± 2.8%, respectively. Computational modeling showed good agreement with the experimental drug release behavior in vitro.Keywords: core-shell nanoparticles, oral formulations, bioavailability, drug delivery, poorly water-soluble drugs, progesterone, poly, lactide-co-glycolide, PLGA, copolymer, coaxial electrospray |
| Databáze: | OpenAIRE |
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