A Hyaluronic Acid Functionalized Self-Nano-Emulsifying Drug Delivery System (SNEDDS) for Enhancement in Ciprofloxacin Targeted Delivery against Intracellular Infection.
A Hyaluronic Acid Functionalized Self-Nano-Emulsifying Drug Delivery System (SNEDDS) for Enhancement in Ciprofloxacin Targeted Delivery against Intracellular Infection.
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DOI：
10.3390/nano11051086
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发表时间：
2021-04-22
期刊：
影响因子：
--
通讯作者：
Pandey S
中科院分区：
文献类型：
--
作者：
Arshad R;Tabish TA;Kiani MH;Ibrahim IM;Shahnaz G;Rahdar A;Kang M;Pandey S
环丙沙星（Ciprofloxacin， CIP）是氟喹诺酮类药物中的一种强效抗菌药物，其溶解度和通透性较差，导致细胞内病原菌产生多重耐药并形成生物膜。为了协同提高CIP的生物制药参数，本研究设计了透明质酸（FDA批准的生物相容性聚合物）功能化的自纳米乳化给药系统（HA-CIP-SNEDDS）。通过溶解度、液滴大小、zeta电位、多分散性指数、热力学稳定性、表面形貌、固态表征、药物加载/释放、细胞摄取和生物相容性对SNEDDS配方进行了测试。最终（HA-CIP-SNEDDS）配方的平均液滴尺寸为50 nm，聚分散指数为0.3，zeta电位为负（- 11.4 mV）。含CIP的ha基SNEDDS对山羊肠道粘液的渗透能力有所提高。4 h后，CIP- snedds与HA-CIP-SNEDDS相比通透性增强了2倍，HA-CIP-SNEDDS的通透性增强了4倍。此外，与游离CIP相比，HA-CIP-SNEDDS具有80%的药物释放优势，持续时间为72 h。然而，HA-CIP-SNEDDS对伤寒沙门菌的抗生物膜活性高于CIP- snedds和游离CIP。与游离CIP相比，HA-CIP-SNEDDS表现出更高的生物相容性和更好的口服药代动力学。综上所述，HA-CIP-SNEDDS制剂似乎是一种很有前景的抗伤寒沙门氏菌制剂，具有很强的靶向潜力。
Ciprofloxacin (CIP), a potent anti-bacterial agent of the fluroquinolone family, shows poor solubility and permeability, thus leading to the development of intracellular pathogens induced multi-drug resistance and biofilms formation. To synergistically improve the biopharmaceutical parameters of CIP, a hyaluronic acid (FDA approved biocompatible polymer) functionalized self-nano emulsifying drug delivery system (HA-CIP-SNEDDS) was designed in the present study. SNEDDS formulations were tested via solubility, droplet size, zeta potential, a polydispersity index, thermodynamic stability, surface morphology, solid-state characterization, drug loading/release, cellular uptake, and biocompatibility. The final (HA-CIP-SNEDDS) formulation exhibited a mean droplet size of 50 nm with the 0.3 poly dispersity index and negative zeta potential (−11.4 mV). HA-based SNEDDS containing CIP showed an improved ability to permeate goat intestinal mucus. After 4 h, CIP-SNEDDS showed a 2-fold and HA-CIP-SNEDDS showed a 4-fold permeation enhancement as compared to the free CIP. Moreover, 80% drug release of HA-CIP-SNEDDS was demonstrated to be superior and sustained for 72 h in comparison to free CIP. However, anti-biofilm activity of HA-CIP-SNEDDS against Salmonella typhi was higher than CIP-SNEDDS and free CIP. HA-CIP-SNEDDS exhibited increased biocompatibility and improved oral pharmacokinetics as compared to free CIP. Taken together, HA-CIP-SNEDDS formulation seems to be a promising agent against Salmonella typhi with a strong targeting potential.
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