Obaidat Rana M, Tashtoush Bassam M, Bayan Mohammad F, Al Bustami Rana T, Alnaief Mohammad
Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
Pharmaceutical Research Unit, Amman, Jordan.
AAPS PharmSciTech. 2015 Dec;16(6):1235-44. doi: 10.1208/s12249-015-0312-2. Epub 2015 Mar 12.
Supercritical fluid technology offers several advantages in preparation of microparticles. These include uniformity in particle size, morphology, and drug distribution without degradation of the product. One of the recent advantages is preparation of porous aerogel carrier with proper aerodynamic properties. In this study, we aimed to prepare chitosan aerogel microparticles using supercritical fluid (SCF) technology and compare that with microparticles produced by freeze drying (FD). Loading the prepared carriers with a model drug (salbutamol) was also performed. Comparisons of the particle properties and physicochemical characterizations were undertaken by evaluating particle size, density, specific surface area, and porosity. In vitro drug release studies were also investigated. The effect of many variables, such as molecular weight of chitosan oligomers, concentrations of chitosan, and concentrations of tripolyphosphate on the release, were also investigated. Chitosan aerogels were efficiently produced by SCF technology with an average particle size of 10 μm with a tapped density values around 0.12 g/mL, specific surface area (73-103) m(2)/g, and porosity (0.20-0.29) cc/g. Whereas, microparticles produced by FD method were characterized as cryogels with larger particle size (64 microns) with clear cracking at the surface. Sustained release profile was achieved for all prepared microparticles of salbutamol produced by the aforementioned methods as compared with pure drug. The results also demonstrates that chitosan molecular weight, polymer concentration, and tripolyphosphate concentration affected the release profile of salbutamol from the prepared microparticles. In conclusion, SCF technology was able to produce chitosan aerogel microparticles loaded with salbutamol that could be suitable for pulmonary drug delivery system.
超临界流体技术在微粒制备方面具有诸多优势。这些优势包括粒径、形态和药物分布的均匀性，且不会使产品降解。近期的优势之一是制备具有适当空气动力学性质的多孔气凝胶载体。在本研究中，我们旨在使用超临界流体（SCF）技术制备壳聚糖气凝胶微粒，并将其与冷冻干燥（FD）法制备的微粒进行比较。还将模型药物（沙丁胺醇）负载到制备的载体上。通过评估粒径、密度、比表面积和孔隙率对微粒性质和物理化学特性进行比较。还研究了体外药物释放。此外，还研究了许多变量，如壳聚糖低聚物的分子量、壳聚糖浓度和三聚磷酸钠浓度对释放的影响。通过SCF技术有效地制备了壳聚糖气凝胶，其平均粒径为10μm，振实密度值约为0.12g/mL，比表面积为（73 - 103）m²/g，孔隙率为（0.20 - 0.29）cc/g。而FD法制备的微粒为冷冻凝胶，粒径较大（64微米），表面有明显裂纹。与纯药物相比，上述方法制备 的所有沙丁胺醇微粒均实现了缓释。结果还表明，壳聚糖分子量、聚合物浓度和三聚磷酸钠浓度影响了沙丁胺醇从制备的微粒中的释放情况。总之，SCF技术能够制备负载沙丁胺醇的壳聚糖气凝胶微粒，适用于肺部给药系统。
