Sahibzada Muhammad Umar Khayam, Sadiq Abdul, Khan Shahzeb, Faidah Hani S, Khurram Muhammad, Amin Muhammad Usman, Haseeb Abdul
Department of Pharmacy, University of Malakand, Chakdara, Lower Dir.
Department of Pharmacy, Sarhad University of Science and Information Technology, Peshawar, Khyber Pakhtunkhwa, Pakistan.
Drug Des Devel Ther. 2017 May 15;11:1453-1464. doi: 10.2147/DDDT.S133806. eCollection 2017.
Silibinin has gained in importance in the past few decades as a hepatoprotector and is used widely as oral therapy for toxic liver damage, liver cirrhosis, and chronic inflammatory liver diseases, as well as for the treatment of different types of cancers. Unfortunately, it has low aqueous solubility and inadequate dissolution, which results in low oral bioavailability.
In this study, nanoparticles (NPs) of silibinin, which is a hydrophobic drug, were manufactured using two cost-effective methods. Antisolvent precipitation with a syringe pump (APSP) and evaporative precipitation of nanosuspension (EPN) were used. The prepared NPs were characterized using different analytical techniques such as scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffractometry (XRD) and were sifted for their bioavailability through in vitro dissolution and solubility studies. Moreover, the prepared NPs were evaluated for antimicrobial activity against a battery of bacteria and yeast.
DSC and XRD studies indicated that the prepared NPs were amorphous in nature, with more solubility and dissolution compared to the crystalline form of this drug. NPs prepared through the EPN method had better results than those prepared using the APSP method. Antimicrobial activities of the NPs were improved compared to the unprocessed drugs, while having comparable activities to standard antimicrobial drugs.
Results indicate that the NPs have significantly increased solubility, dissolution rate, and antimicrobial activities due to the conversion of crystalline structure into amorphous form.
在过去几十年中，水飞蓟宾作为一种肝脏保护剂变得越来越重要，被广泛用作治疗中毒性肝损伤、肝硬化、慢性炎症性肝病以及不同类型癌症的口服药物。不幸的是，它的水溶性低且溶出度不足，导致口服生物利用度低。
在本研究中，使用两种经济有效的方法制备了作为疏水性药物的水飞蓟宾纳米颗粒（NPs）。采用了用注射泵进行的抗溶剂沉淀法（APSP）和纳米混悬液的蒸发沉淀法（EPN）。使用扫描电子显微镜（SEM）、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和X射线粉末衍射法（XRD）等不同分析技术对制备的NPs进行表征，并通过体外溶出度和溶解度研究筛选其生物利用度。此外，对制备的NPs进行了针对一系列细菌和酵母菌的抗菌活性评估。
DSC和XRD研究表明，制备的NPs本质上是无定形的，与该药物的结晶形式相比，具有更高的溶解度和溶出度。通过EPN方法制备的NPs比使用APSP方法制备的NPs具有更好的结果。与未加工的药物相比，NPs的抗菌活性有所提高，同时与标准抗菌药物具有相当的活性。
结果表明，由于晶体结构转变为无定形形式，NPs的溶解度、溶出速率和抗菌活性显著提高。
