Eren Böncü Tuğba, Ozdemir Nurten
Faculty of Pharmacy, Department of Pharmaceutical Technology, Erciyes University, 38280 Kayseri, Turkey.
Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara University, 06560 Ankara, Turkey.
Beilstein J Nanotechnol. 2022 Feb 21;13:245-254. doi: 10.3762/bjnano.13.19. eCollection 2022.
The aim of this study was to produce ampicillin trihydrate-loaded poly(lactic acid) (PLA) and PLA/poly(lactic--glycolic acid) (PLA/PLGA) polymeric nanofibers via electrospinning using 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP) as the solvent for local application in tissue engineering. The effects of ampicillin trihydrate concentration (4-12%) and addition of PLGA (20-80%) on the spinnability of the solutions, morphology, average nanofiber diameter, encapsulation efficiency, drug release, and mechanical properties of PLA and PLA/PLGA nanofibers were examined. All nanofibers were bead-free and uniform. They had favorable encapsulation efficiency (approx. 90%) and mechanical properties. The increase in the amount of ampicillin trihydrate caused an increase in the diameter and burst effect of the nanofibers. The drug release ended on the 7th and 3rd day with nanofibers containing 4% and 12% of drug, respectively. The prolonged and controlled drug release for ten days was obtained with nanofibers containing 8% of drug. Thus, the ideal drug concentration was determined to be 8%. Nanofibers containing PLA/PLGA had a larger diameter than those including PLA. In addition, both the strength and elongation of nanofibers decreased depending on the increase in nanofiber size with the addition of PLGA, increased amount of drug, and ratios of PLGA. Drug release studies showed that PLA/PLGA nanofibers exhibited a lower burst effect and a decrease in drug release when compared to PLA nanofibers. Finally, PLA/PLGA nanofibers can be produced with enhanced encapsulation efficiency and mechanical properties, resulting in controlled and tailored release of ampicillin trihydrate for at least ten days. In conclusion, it was demonstrated that the addition of PLGA in different ratios and the amount of drug can be manipulated to obtain the desired properties (average nanofiber diameter, morphology, in vitro drug release, and mechanical properties) of PLA nanofibers.
本研究的目的是通过静电纺丝法，以1,1,1,3,3,3-六氟-2-丙醇（HFIP）作为溶剂，制备负载三水合氨苄西林的聚乳酸（PLA）和聚乳酸-乙醇酸共聚物（PLA/PLGA）纳米纤维，用于组织工程的局部应用。研究了三水合氨苄西林浓度（4%-12%）和PLGA添加量（20%-80%）对溶液可纺性、形态、纳米纤维平均直径、包封率、药物释放以及PLA和PLA/PLGA纳米纤维力学性能的影响。所有纳米纤维均无珠且均匀。它们具有良好的包封率（约90%）和力学性能。三水合氨苄西林用量的增加导致纳米纤维直径增大和突释效应增强。含4%和12%药物的纳米纤维分别在第7天和第3天药物释放结束。含8%药物的纳米纤维实现了长达10天的延长且可控的药物释放。因此，确定理想的药物浓度为8%。含PLA/PLGA的纳米纤维比含PLA的纳米纤维直径更大。此外，随着PLGA添加量、药物用量增加以及PLGA比例的增加，纳米纤维尺寸增大，其强度和伸长率均降低。药物释放研究表明，与PLA纳米纤维相比，PLA/PLGA纳米纤维的突释效应较低，药物释放量减少。最后，可以制备出具有更高包封率和力学性能的PLA/PLGA纳米纤维，从而实现三水合氨苄西林至少10天的可控和定制释放。总之，研究表明，可以通过控制不同比例的PLGA添加量和药物用量，来获得PLA纳米纤维所需的性能（纳米纤维平均直径、形态、体外药物释放和力学性能）。
