Rheological and Drug Delivery Characteristics of Poloxamer-Based Diclofenac Sodium Formulations for Chronic Wound Site Analgesia.
Rheological and Drug Delivery Characteristics of Poloxamer-Based Diclofenac Sodium Formulations for Chronic Wound Site Analgesia.
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DOI：
10.3390/pharmaceutics12121214
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发表时间：
2020-12-15
期刊：
影响因子：
5.4
通讯作者：
Brogden NK
中科院分区：
文献类型：
--
作者：
Russo J;Fiegel J;Brogden NK
慢性伤口是一个重要的和日益严重的健康问题，临床治疗往往是一个痛苦的经历。局部剂型将是治疗这种疼痛的最佳剂型。泊洛沙姆407是一种热敏性聚合物，在低温下为液体，但在高温下为凝胶，非常适合于对慢性伤口部位施用局部镇痛剂。本研究的目的是评价含双氯芬酸钠的泊洛沙姆407凝胶的凝胶化和药物递送特性，以用于慢性伤口镇痛递送。流变学评价泊洛沙姆制剂的凝胶化性质。使用蛇皮透析膜、完整的猪耳皮肤和通过胶带剥离受损的猪耳皮肤评价了装载有双氯芬酸钠的泊洛沙姆的药物递送性质。使用市售凝胶产品和双氯芬酸钠水溶液作为对照制剂。泊洛沙姆浓度和胶凝温度呈相反变化，并且添加较高浓度的双氯芬酸钠与泊洛沙姆胶凝温度的显著增加相关。泊洛沙姆溶液可有效限制双氯芬酸钠通过屏障性能受损的膜的渗透，泊洛沙姆407的双氯芬酸钠递送与从商业凝胶产品观察到的递送没有显著差异。在24小时内递送的药物量不随泊洛沙姆407浓度的变化而显著变化。本研究的结果表明，泊洛沙姆407可能是一种有用的制剂组分，用于向慢性伤口部位施用止痛产品。
Chronic wounds are a significant and growing health problem, and clinical treatment is often a painful experience. A topical dosage form would be optimal to treat this pain. Poloxamer 407, a thermosensitive polymer that is a liquid at low temperatures but gels at higher temperatures, is well suited to administer topical analgesics to chronic wound sites. The goal of this study was to evaluate the gelation and drug delivery properties of poloxamer 407 gels containing diclofenac sodium for potential use in chronic wound analgesic delivery. The gelation properties of poloxamer formulations were evaluated rheologically. Drug delivery properties of poloxamers loaded with diclofenac sodium were evaluated using snakeskin dialysis membranes, intact porcine ear skin, and porcine ear skin impaired via tape stripping. A commercial gel product and a solution of diclofenac sodium in water were used as control formulations. Poloxamer concentration and gelation temperature varied inversely, and the addition of higher concentrations of diclofenac sodium correlated to significant increases in poloxamer gelation temperature. Poloxamer solutions were effective in limiting the permeation of diclofenac sodium through membranes with impaired barrier properties, and delivery of diclofenac sodium from poloxamer 407 did not vary significantly from delivery observed from the commercial gel product. The amount of drug delivered in 24 h did not change significantly with changes in poloxamer 407 concentration. The results of this study indicate that poloxamer 407 may be a useful formulation component for administration of an analgesic product to a chronic wound site.
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