Mirzaeei Shahla, Mohammadi Ghobad, Fattahi Navid, Mohammadi Pardis, Fattahi Ali, Nikbakht Mohammad Reza, Adibkia Khosro
Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.
Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran.
Adv Pharm Bull. 2019 Jun;9(2):249-254. doi: 10.15171/apb.2019.028. Epub 2019 Jun 1.
The objective of this study was to improve the permeability and water solubility rate of a poor water soluble drug, cyclosporine A (CsA). In order to improve the drug dissolution rate and oral bioavailability, electrospinning method was used as an approach to prepare. The fibers were evaluated for surface morphology, thermal characterizations, drug crystallinity, drug release and bioavailability studies. Scanning electron microscope (SEM) results confirmed that the fibers were in microsize range and the size of the fibers was in the rang of 0.2 to 2 micron. Differential scanning calorimetry (DSC) and powder X-ray diffractometry (XRPD) analysis ensured that the crystalline lattice of drug were weakened or destroyed in the fibers. The drug release was 15.28%, 20.67%, and 32.84% from pure drug, fibers of formulation B, and formulation A, respectively. study results indicated that the bioavailability parameters of the optimized fiber formulation were improved and the maximum concentration (C) were significantly higher for fibers (3001 ng/mL) than for pure drug (2550 ng/mL). The dissolution rate of the formulations was dependent on the nature and ratio of drug to carriers. The physicochemical properties showed that the optimized mixture of polyethylene glycol (PEG) and povidone (PVP) fibers could be an effective carrier for CsA delivery. PEG and PVP fibers improved the absolute bioavailability and drug dissolution rate with appropriate physicochemical properties.
本研究的目的是提高难溶性药物环孢素A（CsA）的渗透性和水溶性速率。为了提高药物的溶出速率和口服生物利用度，采用静电纺丝法进行制备。对纤维进行了表面形态、热特性、药物结晶度、药物释放和生物利用度研究。扫描电子显微镜（SEM）结果证实纤维处于微米尺寸范围，纤维尺寸在0.2至2微米之间。差示扫描量热法（DSC）和粉末X射线衍射法（XRPD）分析确保了药物的晶格在纤维中被削弱或破坏。纯药物、制剂B纤维和制剂A的药物释放率分别为15.28%、20.67%和32.84%。研究结果表明，优化后的纤维制剂的生物利用度参数得到改善，纤维的最大浓度（Cmax）（3001 ng/mL）显著高于纯药物（2550 ng/mL）。制剂的溶出速率取决于药物与载体的性质和比例。物理化学性质表明，聚乙二醇（PEG）和聚维酮（PVP）纤维的优化混合物可能是CsA递送的有效载体。PEG和PVP纤维具有适当的物理化学性质，提高了绝对生物利用度和药物溶出速率。
