Aceclofenac loaded microspheres: Formulation and evaluation of novel preprogrammed drug delivery for the treatment of arthritis

Hema Jaiswal , Mohammad Tahir Ansari , Tarique Mahmood , Farogh Ahsan , Vaseem Ahamad Ansari , Usama Ahmad
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Abstract

Arthritis is a widespread joint disorder globally, the patient completely dependent on NSAIDs which are administered after a fixed interval to subside the pain. This work aims to establish a preprogrammed drug delivery system of aceclofenac with a predetermined lag time for the treatment of arthritis. This new preprogrammed formulation microsphere reduces the time-dependent dose administration as it steadily releases the drug in the blood circulation reducing side effects and increasing patient compliance. Aceclofenac (ACF) loaded polymer microspheres were prepared by a new emulsification and crosslinking method using glutaraldehyde as cross-linking agent. Microspheres were prepared in 6 batches using different polymers like sodium alginate, guar gum and chitosan, alone, as well as in combinations. The type and quantity of polymers were changed in every batch while the amount of aceclofenac was unvarying. The microspheres were then evaluated for the particle size, drug content, percentage yield, percentage entrapment efficiency and percentage drug release followed by noting the lag time. The microsphere loaded with aceclofenac were formulated and evaluated, the result showed that all the preparations showed a good lag time (2–3 ​h), but chitosan (alone) gave the highest lag time, which fulfills the aim of pre-programmed drug delivery system. Preprogrammed drug release has been achieved from the microspheres over a period of 0–7 ​h, consistent with the demand for chronotherapeutic drug delivery for the treatment of arthritis. The major signification of the preparation technique includes short processing time and the lack of exposure of the ingredients to high temperatures. Aceclofenac-loaded microspheres offer a promising avenue for arthritis treatment, ensuring sustained drug release. Their potential clinical implications include enhanced therapeutic efficacy, reduced side effects, and improved patient compliance. Future directions may involve personalized formulations, targeted delivery systems, and exploring applications beyond arthritis, expanding the scope of this innovative drug delivery approach.

醋氯芬酸负载微球:用于治疗关节炎的新型预编程给药的制备与评估
关节炎是全球广泛存在的一种关节疾病,患者完全依赖非甾体抗炎药物在固定时间间隔后给药来缓解疼痛。这项研究旨在建立一种具有预定滞后时间的醋氯芬酸预编程给药系统,用于治疗关节炎。这种新的预编程配方微球减少了剂量给药的时间依赖性,因为它能在血液循环中稳定释放药物,从而减少副作用并提高患者的依从性。使用戊二醛作为交联剂,通过一种新的乳化和交联方法制备了负载醋氯芬酸(ACF)的聚合物微球。使用海藻酸钠、瓜尔豆胶和壳聚糖等不同聚合物单独或组合制备了 6 批微球。每批聚合物的类型和数量都有所变化,而醋氯芬酸的用量则保持不变。然后对微球的粒度、药物含量、产量百分比、夹持效率百分比和药物释放百分比进行评估,并记录滞后时间。结果表明,所有制剂都显示出良好的滞后时间(2-3 小时),但壳聚糖(单独)的滞后时间最长,达到了预编程给药系统的目的。微球在 0-7 小时内实现了预编程药物释放,符合治疗关节炎的时程给药需求。这种制备技术的主要特点是加工时间短,成分无需暴露在高温下。装载醋氯芬酸的微球为关节炎治疗提供了一种前景广阔的途径,可确保药物的持续释放。其潜在的临床意义包括提高疗效、减少副作用和改善患者的依从性。未来的发展方向可能包括个性化配方、靶向给药系统以及探索关节炎以外的应用,从而扩大这种创新给药方法的应用范围。
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