학술논문
Tween 80-Based Self-Assembled Mixed Micelles Boost Valsartan Transdermal Delivery.
Document Type
Academic Journal
Author
Yassin AEB; College of Pharmacy, King Abdullah International Medical Research Center, King Saud Bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.; Massadeh S; Developmental Medicine Department, King Abdullah International Medical Research Center, King Saud Bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.; Joint Centers of Excellence Program, KACST-BWH/Harvard Center of Excellence for Biomedicine, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi Arabia.; Alshwaimi AA; AstraZeneca Saudi Arabia, Riyadh 13315, Saudi Arabia.; Kittaneh RH; Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus P400, Palestine.; Omer ME; Pharmacy Program, College of Health and Sport Sciences, University of Bahrain, Manama 32038, Bahrain.; Ahmad D; College of Pharmacy, King Abdullah International Medical Research Center, King Saud Bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.; Aodah AH; Advanced Diagnostic and Therapeutic Institute, Health Sector, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi Arabia.; Shakeel F; Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.; Halwani M; Nanomedicine Department, King Abdullah International Medical Research Center, King Saud Bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.; Alanazi SA; College of Pharmacy, King Abdullah International Medical Research Center, King Saud Bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.; Pharmaceutical Care Services, King Abdulaziz Medical City, National Guard Health Affairs (NGHA), Riyadh 11426, Saudi Arabia.; Alam P; Department of Pharmacognosy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
Source
Publisher: MDPI Country of Publication: Switzerland NLM ID: 101238453 Publication Model: Electronic Cited Medium: Print ISSN: 1424-8247 (Print) Linking ISSN: 14248247 NLM ISO Abbreviation: Pharmaceuticals (Basel) Subsets: PubMed not MEDLINE
Subject
Language
English
ISSN
1424-8247
Abstract
Valsartan (Val) is an important antihypertensive medication with poor absorption and low oral bioavailability. These constraints are due to its poor solubility and dissolution rate. The purpose of this study was to optimize a mixed micelle system for the transdermal delivery of Val in order to improve its therapeutic performance by providing prolonged uniform drug levels while minimizing drug side effects. Thin-film hydration and micro-phase separation were used to produce Val-loaded mixed micelle systems. A variety of factors, including the surfactant type and drug-to-surfactant ratio, were optimized to produce micelles with a low size and high Val entrapment efficiency (EE). The size, polydispersity index (PDI), zeta potential, and drug EE of the prepared micelles were all measured. The in vitro drug release profiles were assessed using dialysis bags, and the permeation through abdominal rat skin was assessed using a Franz diffusion cell. All formulations had high EE levels exceeding 90% and low particle charges. The micellar sizes ranged from 107.6 to 191.7 nm, with average PDI values of 0.3. The in vitro release demonstrated a uniform slow rate that lasted one week with varying extents. F7 demonstrated a significant ( p < 0.01) transdermal efflux of 68.84 ± 3.96 µg/cm 2 /h through rat skin when compared to the control. As a result, the enhancement factor was 16.57. In summary, Val-loaded mixed micelles were successfully prepared using two simple methods with high reproducibility, and extensive transdermal delivery was demonstrated in the absence of any aggressive skin-modifying enhancers.