Hendradi Esti, Hariyadi Dewi Melani, Adrianto Muhammad Faris
Department of Pharmaceutics, Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia.
Res Pharm Sci. 2018 Feb;13(1):38-46. doi: 10.4103/1735-5362.220966.
The objective of this study was to determine and evaluate a controlled release implant of ciprofloxacin using bovine hydroxyapatite (BHA)-chitosan composite and glutaraldehyde or genipin as crosslinking agents. Ciprofloxacin implants were prepared using BHA, chitosan, ciprofloxacin at 30:60:10 and using three different concentrations of glutaraldehyde or genipin (0.3, 0.5, or 0.7%) as crosslinkers. Implants were formed as mini-tablet with 4.0 mm diameter weighing 100 mg using compression method. Further, the prepared ciprofloxacin implants were characterized for porosity, density, water absorption capacity, swelling, degradation, compressive strength, compatibility (Fourier transforms-infrared spectroscopy (FT-IR)), morphology (scanning electron microscope (SEM)), X-ray diffraction (X-RD), and drug release. The addition of glutaraldehyde or genipin as crosslinkers in ciprofloxacin implant showed controlled release profile of ciprofloxacin over a time period of 30 days. SEM photomicrograph revealed low porosity of the implant after crosslinking with glutaraldehyde or genipin. The FTIR study confirmed the formation of covalent imine bonds between chitosan and glutaraldehyde. Moreover, the addition of glutaraldehyde or genipin as crosslinkers caused a decrease in the mechanical strength of the implant. Increased concentration of glutaraldehyde or genipin reduced the crystallinity of BHA and chitosan, which were confirmed by X-RD studies. The results obtained from this study indicated that glutaraldehyde or genipin had the potential effect to retard ciprofloxacin release from BHA-chitosan-ciprofloxacin implant for 30 days.
本研究的目的是确定并评估一种使用牛羟基磷灰石（BHA）-壳聚糖复合材料以及戊二醛或京尼平作为交联剂的环丙沙星控释植入物。使用BHA、壳聚糖、环丙沙星按30:60:10的比例，并使用三种不同浓度的戊二醛或京尼平（0.3%、0.5%或0.7%）作为交联剂来制备环丙沙星植入物。采用压制法将植入物制成直径4.0毫米、重100毫克的微型片剂。此外，对制备的环丙沙星植入物进行孔隙率、密度、吸水能力、溶胀、降解、抗压强度、相容性（傅里叶变换红外光谱（FT-IR））、形态（扫描电子显微镜（SEM））、X射线衍射（X-RD）以及药物释放等方面的表征。在环丙沙星植入物中添加戊二醛或京尼平作为交联剂后，环丙沙星在30天的时间段内呈现出控释特性。SEM显微照片显示，与戊二醛或京尼平交联后的植入物孔隙率较低。FTIR研究证实壳聚糖与戊二醛之间形成了共价亚胺键。此外，添加戊二醛或京尼平作为交联剂会导致植入物的机械强度降低。X-RD研究证实，戊二醛或京尼平浓度的增加会降低BHA和壳聚糖的结晶度。本研究获得的结果表明，戊二醛或京尼平具有使环丙沙星从BHA-壳聚糖-环丙沙星植入物中缓释30天的潜在作用。
