College of Pharmacy, Weifang Medical University, Weifang 261053, Shandong, China.
Weifang Maternity and Child Care Hospital, Weifang 261053, Shandong, China.
Biomed Res Int. 2018 Jul 24;2018:9073420. doi: 10.1155/2018/9073420. eCollection 2018.
Proanthocyanidin (PC) has attracted wide attention on cosmetics and pharmaceutical due to its antioxidant, anticancer, antimicrobial, antiangiogenic, and anti-inflammatory activities. However, PC applications are limited because of its sensitivity to thermal treatment, light, and oxidation and the poor absorption in the gastrointestinal tract. Thus, a novel dosage form of PC needs to be designed to improve its stability and bioavailability for drug delivery. The objective of this study is to fabricate proanthocyanidins/chitosan/lecithin (PC/CTS/LEC) microspheres and investigate various characteristics. In the current study, PC/CTS/LEC microspheres were prepared by spray-drying technology. The yield (61.68%), encapsulation efficiency (68.19%), and drug loading capacity (17.05%) were found in the results. The scanning electron microscope demonstrated that the microspheres were spherical in shape with wrinkled surfaces. DSC study displayed that the microspheres stability was greatly improved when comparing with bare PC. The in vitro release study showed that the 76.92% of PC was released from microspheres within 48 h. The moisture contents of microspheres ranged from 8% to 13%. The swelling rate and tapped density of microspheres were elevated with increasing the concentration of chitosan in the formulations. The moisture uptake of microspheres was saturated at 40°C/RH75% within 12 h. Our results indicated that the stability of PC/CTS/LEC microspheres was enhanced, and it is a promising carrier for sustained drug delivery system.
原花青素（PC）因其抗氧化、抗癌、抗菌、抗血管生成和抗炎活性而在化妆品和制药领域引起了广泛关注。然而，由于其对热处理、光和氧化的敏感性以及在胃肠道中的吸收不良，PC 的应用受到限制。因此，需要设计一种新的 PC 剂型，以提高其稳定性和生物利用度，用于药物输送。本研究的目的是制备原花青素/壳聚糖/卵磷脂（PC/CTS/LEC）微球并研究其各种特性。在目前的研究中，PC/CTS/LEC 微球是通过喷雾干燥技术制备的。结果发现，产率（61.68%）、包封效率（68.19%）和载药量（17.05%）。扫描电子显微镜表明，微球呈球形，表面有皱纹。DSC 研究表明，与原 PC 相比，微球的稳定性大大提高。体外释放研究表明，76.92%的 PC 在 48 小时内从微球中释放出来。微球的水分含量在 8%至 13%之间。随着配方中壳聚糖浓度的增加，微球的溶胀率和振实密度升高。微球的吸湿性在 40°C/RH75%下 12 小时内达到饱和。我们的结果表明，PC/CTS/LEC 微球的稳定性得到了增强，是一种有前途的持续药物输送系统载体。
