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Design and Development of a novel transmucosal patch Embedded with Diclofenac Diethylamine loaded solid lipid nanoparticles

机译:新型双粘膜二乙胺固体脂质纳米粒包埋的透粘膜贴剂的设计与开发

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Objective: Diclofenac diethylamine (DDEA) loaded solid lipid nanoparticles (SLN) were developed and incorporated in to transmucosal patch (TP) for application in dental surgeries. Methods: DDEA-SLNs were prepared by solvent emulsion evaporation method with compritol 888 ATO as lipid and soya lecithin, Pluronic F68 as surfactants and optimized by a 3-factor 3-level central composite design for its impact on particle size (PS) and entrapment efficiency (EE). SLN was incorporated into a bilayer TP prepared with hydroxypropyl cellulose – LF and polycarbophil along with Labrafac as plasticizer. TP was characterized for tensile and mucoadhesive strength, FTIR, DSC, XRD, SEM, in vitro and ex vivo release. Results: PS, EE, in vitro and ex vivo release of the optimized SLN batch D6 were found to be 178.88 ± 1.3 nm, 54.14 ± 1.6%, 98.26 ± 3.4% and 96.28 ± 3.5% at 24 h respectively. TP showed 99.22 ± 0.7% of in vitro release and 99.53 ± 0.9% permeation through porcine mucosa at 24 h with satisfactory tensile strength and mucoadhesive properties. Conclusion: The designed once a day TP loaded with DDEA-SLN applied at the gingival site, immediately after dental surgery has the potential to produce therapeutic relief locally which is prolonged for 24 h, with the added advantage of overcoming first pass metabolism and gastric irritation, in addition to decreasing the frequency of administration of Diclofenac.
机译:目的:开发了负载双氯芬酸二乙胺(DDEA)的固体脂质纳米颗粒(SLN),并将其掺入透粘膜贴剂(TP)中,以用于牙科手术。方法:采用溶剂乳化蒸发法,以Compritol 888 ATO为脂质,大豆卵磷脂,Pluronic F68为表面活性剂,通过三因素三级中心复合设计优化了DDEA-SLNs对粒径和包封率的影响。效率(EE)。 SLN被掺入双层TP中,该双层TP由羟丙基纤维素– LF和聚卡波非与Labrafac作为增塑剂一起制备。 TP的抗张强度和粘膜粘附强度,FTIR,DSC,XRD,SEM,体外和离体释放均经过表征。结果:优化后的SLN批次D6的PS,EE,体外和离体释放在24 h分别为178.88±1.3 nm,54.14±1.6%,98.26±3.4%和96.28±3.5%。 TP在24 h时显示出99.22±0.7%的体外释放和99.53±0.9%的猪粘膜渗透性,具有令人满意的拉伸强度和粘膜粘附特性​​。结论:在牙科手术后立即设计的每日一次在牙龈部位应用DDEA-SLN的TP具有潜在的局部缓解作用,可延长24 h,具有克服首过代谢和胃刺激的优势。 ,除了减少双氯芬酸的给药频率。

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