地塞米松负载电纺纳米复合材料眼内植入物的体外药物释放和力学评价

R. Agarwal, Dhwani Rana, Sagar Salave, Derajram Benival
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引用次数: 1

摘要

地塞米松目前可作为眼前炎性疾病的悬浮液,通过滴眼液给予治疗。当局部滴眼液时,不到5%的药物被吸收。给药的大部分药物要么从眼睛流出,要么通过鼻泪引流,导致生物利用度差。本研究旨在利用静电纺丝技术开发含地塞米松的聚合物眼植入物。在乙醇:水(90:10)的溶剂体系中,以10% w/v EC: HPMC: PEO(60:20:20)为负载地塞米松(0.1% w/v)的静电纺丝片,最佳静电纺丝参数为12kV,流速为0.8mL/hr,针尖与捕集剂之间的距离为20cm。用DSC和FTIR-ATR对制备的纳米复合插入物进行了表征,发现药物与聚合物之间没有物理化学相互作用。电纺丝片的厚度为270±0.02 μm,药物含量为0.43±0.01% w/w。释放谱显示,约95%的药物在48小时内释放。该释放谱显示所制备的载药电纺丝眼植入物最适合每天一次给药。杨氏模量、抗拉强度和伸长率等机械性能的评估表明,制备的插入物可以很容易地处理,没有任何断裂或损坏。在结膜囊内分娩时,最适合每天一次分娩。所开发的电纺丝插入物由一种独特的可生物降解聚合物复合材料组成,利用纳米纤维延长释放的优点,这种新配方克服了传统疗法的局限性。这减少了给药频率,提高了患者的依从性。
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Dexamethasone Loaded Electrospun Nanocomposite Ocular Insert: In-vitro Drug Release and Mechanical Assessment
Dexamethasone is currently available as suspension for the treatment of anterior ocular inflammatory diseases that are given through eye drops. Upon topical delivery by eye-drops, less than 5% of the drug gets absorbed when applied topically as eye drops. The major portion of administered drug either comes out from the eye or gets subjected to nasolacrimal drainage resulting in poor bioavailability. The present study is aimed at developing polymeric ocular insert containing dexamethasone as a drug by employing the use of electrospinning technique. Dexamethasone (0.1% w/v) loaded electrospun sheet was also made using 10% w/v EC: HPMC: PEO (60:20:20) in solvent system of ethanol: water (90:10) at optimized electrospinning parameters of 12kV with a flow rate of 0.8mL/hr and distance of 20 cm between tip and collector. The prepared nanocomposite insert was characterized for DSC and FTIR-ATR spectroscopy revealing no physical-chemical interaction between drug with polymers. The thickness of the electrospun sheet was found to be 270±0.02 μm and % drug content was found to be 0.43±0.01% w/w. The release profile showed that around 95% drug was released in 48 hrs. This release profile showed the prepared drug-loaded electrospun ocular insert was best suitable for once-a-day delivery. Assessment of mechanical properties like young’s modulus, tensile strength, and % elongation showed that the prepared insert can be handled easily without any breakage or damage. Upon delivery in conjunctival sac, this is best suitable for once-a-day delivery. The developed electrospun insert, consisting of a unique polymer composite of biodegradable polymers, avails the benefits of nanofibers imparting prolonged release and this novel formulation overcomes the limitations of conventional therapies. This reduces the dosing frequency and improves patient compliance.
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来源期刊
Current Nanomedicine
Current Nanomedicine Medicine-Medicine (miscellaneous)
CiteScore
2.00
自引率
0.00%
发文量
15
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