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Electrostatic spraying for fine-tuning particle dimensions to enhance oral bioavailability of poorly water-soluble drugs

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Asian Journal of Pharmaceutical Sciences 2024年第5期19卷 139-151页

作者： Jung Suk Kim seunghyun cheon Mi RanWoo Sanghyun Woo Jee-Eun Chung Yu Seok Youn Kyung Taek Oh Soo-Jeong Lim Sae Kwang Ku Bao LoNguyen Jong Oh Kim Sung Giu Jin Han-Gon Choi College of Pharmacy Hanyang UniversityAnsan 15588South Korea School of Pharmacy Sungkyunkwan UniversitySuwon 440746South Korea College of Pharmacy Chung-Ang UniversitySeoul 156-756South Korea Department of Bioscience and biotechnology Sejong UniversitySeoul 143747South Korea Department of Anatomy and Histology College of Korean MedicineDaegu Haany UniversityGyeongsan 38610South Korea College of Pharmacy Yeungnam UniversityGyongsan 712749South Korea Department of Pharmaceutical Engineering Dankook UniversityCheonan 31116South Korea

While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs,the outcomes often exhibit suboptimal particle size distribution and large particle sizes,limiting their *** this study,we introduce electrostatic spraying as an advanced technology tailored for poorly water-soluble drugs,enabling the fabrication of nanoparticles with fine and uniform particle size ***(1 g),as a model drug,copovidone(5 g),and sodium dodecyl sulfate(0.1 g)were dissolved in 200 ml ethanol and subjected to conventional-spray-dryer and electrostatic spray *** electrostatic spray-dried nanoparticles(ESDN)showed smaller particle sizes with better uniformity compared to conventional spray-dried nanoparticles(CSDN).ESDN demonstrated significantly enhanced solubility and rapid release in *** vitro studies revealed that ESDN induced apoptosis in HCT-116 cells to a greater extent,exhibiting superior cytotoxicity compared to ***,ESDN substantially improved oral bioavailability and antitumor efficacy compared to *** findings suggest that ESD shows potential in developing enhanced drug delivery systems for poorly water-soluble drugs,effectively addressing the limitations associated with CSD methods.

关键词： Electrostatic spray drying Poorly water-soluble drug Regorafenib Particle size distribution Oral bioavailability Oral antitumor efficacy

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