Department of Pharmaceutics, College of Pharmacy, Al- Qassim University, Buraidah, Kingdom of Saudi Arabia.
College of Pharmacy, Al- Qassim University, Buraidah, Kingdom of Saudi Arabia.
Drug Des Devel Ther. 2021 Jul 2;15:2869-2884. doi: 10.2147/DDDT.S309078. eCollection 2021.
The aim of the work was to formulate salbutamol sulfate (SB) microspheres by using superhydrophobic surface (SHS) under different processing factors for improving its encapsulation efficiency, controling its release rate, and hence enhancing its bioavailability.
Cross-linked microspheres of chitosan (CN) and carrageenan (KN) were made on a SHS under a glutaraldehyde-saturated atmosphere. The formulations were designed and optimized based on 4 factorial design. Percentage encapsulation efficiency (%EE), particle size, swelling ratio, and in vitro release rate were characterized, and the in vivo performance of optimized formula was investigated in beagle dogs.
The results showed that the prepared microspheres have a high %EE (97.11±0.78%) for F13. The swelling ratio was 4.2 at the end of the 8 hours for the optimized formula, and the in vitro release rate was controlled for 12 hours. In vivo study verified that there was a 1.61-fold enhancement in SB bioavailability from optimized formula (F13) compared to market tablet.
The study suggested that microspheres prepared from CN/KN crosslinking on an SHS using glutaraldehyde atmosphere is a promising technique that can encapsulate and sustain the release of water-soluble drugs such as SB in addition to improving its in vivo pharmacokinetic profile.
本工作旨在通过使用超疏水表面（SHS）在不同的加工因素下制备硫酸沙丁胺醇（SB）微球，以提高其包封效率、控制其释放速率，从而提高其生物利用度。
壳聚糖（CN）和卡拉胶（KN）的交联微球在戊二醛饱和气氛下的 SHS 上形成。根据 4 因素设计进行配方设计和优化。表征包封效率（%EE）、粒径、溶胀比和体外释放率，并在比格犬中研究优化配方的体内性能。
结果表明，所制备的微球具有高的%EE（97.11±0.78%），对于 F13。优化配方在 8 小时结束时的溶胀比为 4.2，体外释放速率可控制 12 小时。体内研究证实，与市售片剂相比，优化配方（F13）使 SB 的生物利用度提高了 1.61 倍。
研究表明，使用戊二醛气氛在 SHS 上交联 CN/KN 制备的微球是一种有前途的技术，除了改善其体内药代动力学特征外，还可以包封和持续释放水溶性药物，如 SB。
