Aceclofenac ethosomes for enhanced transdermal delivery

S. Lewis, V. Dave
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引用次数: 2

Abstract

The oral administration of aceclofenac has often resulted in side effects with chronic use. Using the transdermal route eliminates these side effects. Aceclofenac ethosomes were prepared and incorporated into a gel to enhance the skin permeability of aceclofenac. Ethosomal system comprised of phospholipids, ethanol, propylene glycol and lecithin. Different formulations were prepared with varying concentrations of lecithin and ethanol. The optical microscopy confirmed the formulation of multilamellar vesicles. The vesicle size of the ethosomes ranged between 0.696–1.140µm. Surface morphology was conducted by scanning electron microscopy. The entrapment efficiency was determined by centrifugation method. Effect of ethanol and lecithin concentration on entrapment of ethosomes was observed. Franz diffusion cell was used to evaluate the in vitro transdermal permeability of aceclofenac ethosomes. The studies were carried out using mouse skin as well as commercial sigma membrane. The in vitro drug permeation of the optimised formulation was compared with commercial conventional gel-Ziynac gel. The flux values of different ethosomal formulation were observed between 116.5µg/cm2/hr to 226.15µg/cm2 /hr. Formulation 5 showed maximum J value 226.1 as compared to marketed one 131.5µg/cm2 /hr. From the results of the present study it can be concluded that ethosomes improve the transdermal flux, prolong the release and represent an active carrier for sustained transdermal delivery.
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乙酰氯芬酸溶酶体增强透皮给药
长期口服乙酰氯芬酸常常导致副作用。使用透皮途径消除了这些副作用。制备乙酰氯芬酸脂质体并将其掺入凝胶中,以增强乙酰氯芬酸的皮肤渗透性。由磷脂、乙醇、丙二醇和卵磷脂组成的醇体系统。用不同浓度的卵磷脂和乙醇制备了不同的配方。光学显微镜证实了多层囊泡的形成。酶质体的囊泡大小在0.696 ~ 1.140µm之间。用扫描电镜观察表面形貌。采用离心法测定包封效率。观察了乙醇和卵磷脂浓度对酶体包埋的影响。采用Franz扩散池评价乙酰氯芬酸脂质体的体外透皮渗透性。研究采用小鼠皮肤和商业sigma膜进行。并与市售常规凝胶ziynac凝胶进行了体外药物透性比较。不同制剂的通量值在116.5µg/cm2/hr ~ 226.15µg/cm2 /hr之间。与市售的131.5µg/cm2 /hr相比,配方5的最大J值为226.1。从本研究的结果可以得出结论,脂质体提高透皮通量,延长释放时间,是持续透皮给药的有效载体。
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