{"title":"增强乙酰氯芬酸经皮给药的酶体","authors":"V. Dave, Dhirendra Kumar, S. Lewis, S. Paliwal","doi":"10.5138/IJDD.2010.0975.0215.02016","DOIUrl":null,"url":null,"abstract":"The aim of the current investigation is to evaluate the transdermal potential of novel vesicular carrier, ethosomes, bearing aceclofenac, Non-steroidal anti-inflammatory drugs (NSAIDs) agents having limited transdermal permeation. Aceclofenac loaded ethosomal carriers were prepared, optimized and characterized for vesicular shape and surface morphology,(SEM) scanning electronic microscopy, vesicular size, entrapment efficiency, stability, in- vitro release study. The formulation (Etho5) having 3% phospholipids contant and 40% ethanol showing the grater entrapment (93.3%) and optimal average vesicle size of formulation (Etho5) determine by Malvern Zetamaster ZEM & 0.696μm and zeta potential of formulation was -6.74 mV. The formulation (Etho12) having 3% phospholipids contant and 40% isopropyl alcohol showing the grater entrapment (95.7%). stability profile of prepared system assessed for 45 days. The vesicular suspension was kept in sealed vials (10ml) at 4 ± 2oC and at room temperature for 45 days no change is shown in the entrapment efficiency. The optimized ethosomal formulation showed transdermal flux (226.1 μg/cm²/hr) for ethanolic drug solution which is grater then that of isopropyl alcohol solution (159.0 μg/cm²/hr). The result advocates the potential of ethosome formulation to treat rheumatic disease where facilitated penetration of the drug into muscle and synovial fluid is desirable. In light of the data obtained from experimental work we can expect the ethosome formulation to be safe and very efficient as a drug carrier for systemic as well as topical delivery of drug, holding future in effective transdermal delivery. 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Aceclofenac loaded ethosomal carriers were prepared, optimized and characterized for vesicular shape and surface morphology,(SEM) scanning electronic microscopy, vesicular size, entrapment efficiency, stability, in- vitro release study. The formulation (Etho5) having 3% phospholipids contant and 40% ethanol showing the grater entrapment (93.3%) and optimal average vesicle size of formulation (Etho5) determine by Malvern Zetamaster ZEM & 0.696μm and zeta potential of formulation was -6.74 mV. The formulation (Etho12) having 3% phospholipids contant and 40% isopropyl alcohol showing the grater entrapment (95.7%). stability profile of prepared system assessed for 45 days. The vesicular suspension was kept in sealed vials (10ml) at 4 ± 2oC and at room temperature for 45 days no change is shown in the entrapment efficiency. The optimized ethosomal formulation showed transdermal flux (226.1 μg/cm²/hr) for ethanolic drug solution which is grater then that of isopropyl alcohol solution (159.0 μg/cm²/hr). The result advocates the potential of ethosome formulation to treat rheumatic disease where facilitated penetration of the drug into muscle and synovial fluid is desirable. In light of the data obtained from experimental work we can expect the ethosome formulation to be safe and very efficient as a drug carrier for systemic as well as topical delivery of drug, holding future in effective transdermal delivery. 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引用次数: 83
摘要
本研究的目的是评估新型囊泡载体,溶酶体,含乙酰氯芬酸,非甾体抗炎药(NSAIDs)药物的透皮渗透有限。制备并优化了乙酰氯芬酸载体载体,并对其进行了囊泡形状、表面形貌、扫描电镜(SEM)、囊泡大小、包封效率、稳定性、体外释放研究。采用Malvern Zetamaster ZEM & 0.696μm测定了磷脂含量为3%、乙醇含量为40%的配方(Etho5)的包封率为93.3%,最佳平均囊泡大小为-6.74 mV, zeta电位为-6.74 mV。含有3%磷脂和40%异丙醇的配方(Etho12)显示出更大的包裹度(95.7%)。对制备的体系进行了45天的稳定性评估。囊泡悬浮液在4±20℃和室温下密封瓶(10ml)保存45天,包封效率无变化。优化后的乙醇溶液的透皮通量为226.1 μg/cm²/hr,大于异丙醇溶液的159.0 μg/cm²/hr。该结果提倡溶酶体制剂治疗风湿性疾病的潜力,其中促进药物渗透到肌肉和滑液是可取的。根据从实验工作中获得的数据,我们可以预期,乙醇体制剂作为药物载体,无论是全身还是局部给药,都是安全高效的,在有效的透皮给药方面具有广阔的前景。关键词:Ethosome;Aceclofenac;磷脂;经皮的
Ethosome for Enhanced Transdermal Drug Delivery of Aceclofenac
The aim of the current investigation is to evaluate the transdermal potential of novel vesicular carrier, ethosomes, bearing aceclofenac, Non-steroidal anti-inflammatory drugs (NSAIDs) agents having limited transdermal permeation. Aceclofenac loaded ethosomal carriers were prepared, optimized and characterized for vesicular shape and surface morphology,(SEM) scanning electronic microscopy, vesicular size, entrapment efficiency, stability, in- vitro release study. The formulation (Etho5) having 3% phospholipids contant and 40% ethanol showing the grater entrapment (93.3%) and optimal average vesicle size of formulation (Etho5) determine by Malvern Zetamaster ZEM & 0.696μm and zeta potential of formulation was -6.74 mV. The formulation (Etho12) having 3% phospholipids contant and 40% isopropyl alcohol showing the grater entrapment (95.7%). stability profile of prepared system assessed for 45 days. The vesicular suspension was kept in sealed vials (10ml) at 4 ± 2oC and at room temperature for 45 days no change is shown in the entrapment efficiency. The optimized ethosomal formulation showed transdermal flux (226.1 μg/cm²/hr) for ethanolic drug solution which is grater then that of isopropyl alcohol solution (159.0 μg/cm²/hr). The result advocates the potential of ethosome formulation to treat rheumatic disease where facilitated penetration of the drug into muscle and synovial fluid is desirable. In light of the data obtained from experimental work we can expect the ethosome formulation to be safe and very efficient as a drug carrier for systemic as well as topical delivery of drug, holding future in effective transdermal delivery. Keywords: Ethosome; Aceclofenac; Phospholipid; Transdermal