Bashir Kashaf, Khan Muhammad Farhan Ali, Alhodaib Aiyeshah, Ahmed Naveed, Naz Iffat, Mirza Bushra, Tipu Muhammad Khalid, Fatima Humaira
Department of Pharmacy, Quaid-i-Azam University, Islamabad 45320, Pakistan.
Department of Physics, College of Science, Qassim University, Buraydah 51452, Saudi Arabia.
Polymers (Basel). 2022 Apr 19;14(9):1639. doi: 10.3390/polym14091639.
The aim of the current study is extraction and isolation of bergenin from and fabrication of pH-sensitive Eudragit L100 (EL100) polymeric nanoparticles (NP) to tackle limitations of solubility. Bergenin-loaded EL100 nanoparticles (BN-NP) were fabricated via nanoprecipitation and an experimental design was conducted for optimization. A reverse phase-high performance liquid chromatography (RP-HPLC) method was developed for the quantitation of bergenin. The optimized nanoformulation was characterized by its particle size, morphology, loading capacity, entrapment efficiency, drug-excipient interaction and crystallinity. An in vitro assay was executed to gauge the release potential of pH-sensitive nanoformulation. The mean particle size, zeta potential and polydispersity index (PDI) of the optimized nanoparticles were observed to be 86.17 ± 2.1 nm, -32.33 ± 5.53 mV and 0.30 ± 0.03, respectively. The morphological analysis confirmed the spherical nature of the nanoparticles. Drug loading capacity and entrapment efficiency were calculated to be 16 ± 0.34% and 84 ± 1.3%, respectively. Fourier transform infrared spectroscopy (FTIR) studies unfolded that no interaction was present between the drug and the excipients in the nanoformulation. Crystallography studies revealed that the crystalline nature of bergenin was changed to amorphous and the nanoformulation was stable for up to 3 months at 40 °C. The present study confirms that bergenin isolation can be scaled up from abundantly growing . Moreover, it could also be delivered by entrapment in stimuli-responsive polymer, preventing the loss of drug in healthy tissues.
本研究的目的是从[具体来源未给出]中提取和分离岩白菜素，并制备对pH敏感的聚丙烯酸树脂L100（EL100）聚合物纳米颗粒（NP），以解决其溶解度限制问题。通过纳米沉淀法制备了载岩白菜素的EL100纳米颗粒（BN-NP），并进行了实验设计以优化其性能。开发了一种反相高效液相色谱（RP-HPLC）方法用于岩白菜素的定量分析。通过粒径、形态、载药量、包封率、药物-辅料相互作用和结晶度对优化后的纳米制剂进行了表征。进行了体外试验以评估pH敏感纳米制剂的释放潜力。优化后的纳米颗粒的平均粒径、zeta电位和多分散指数（PDI）分别为86.17±2.1nm、-32.33±5.53mV和0.30±0.03。形态分析证实了纳米颗粒的球形性质。载药量和包封率分别计算为16±0.34%和84±1.3%。傅里叶变换红外光谱（FTIR）研究表明，纳米制剂中药物与辅料之间不存在相互作用。晶体学研究表明，岩白菜素的晶体性质转变为无定形，并且该纳米制剂在40℃下可稳定保存3个月。本研究证实，岩白菜素的分离可以从大量生长的[具体来源未给出]中扩大规模。此外，它还可以通过包裹在刺激响应性聚合物中来递送，从而防止药物在健康组织中流失。
