Retention enhancement

  • 文章类型: Journal Article
    这项研究旨在创造一个低负荷,高保留,使用化学增强剂(CE)方法更容易应用O/W糠酸莫米松(MF)乳膏,为特应性皮炎(AD)患者提供更多选择,并研究其释放和保留增加的分子机制。Box-Behnken设计基于稳定性和体外皮肤保留确定了最佳配方。评估包括外观,流变性能,刺激,体内组织分布和药效学。使用高速离心法研究了增强释放的分子机制,分子动力学和流变学。CE之间的相互作用,通过胶带剥离研究了MF和皮肤,CLSM,ATR-FTIR和SAXS。优化配方以含有0.05%MF,并使用10%聚甘油-3油酸酯(POCC)作为CE。与Elocon®乳膏在体内保留和药效学方面没有显著差异,但与基础制剂相比,体内保留增加3.14倍,体外释放增加1.77倍。POCC降低了油相内聚能密度,增强药物的流动性和释放。它破坏了皮肤脂质相,帮助药物进入并形成氢键,延长保留时间。这项研究强调了POCC作为奶油中的CE,为半固体制剂的开发提供见解。
    The study aimed to create a low loading, high retention, easier to apply O/W mometasone furoate (MF) cream using a chemical enhancer (CE) approach to provide more options for patients with atopic dermatitis (AD) and to investigate molecular mechanisms of its increased release and retention. A Box-Behnken design determined the optimal formulation based on stability and in vitro skin retention. Evaluations included appearance, rheological properties, irritation, in vivo tissue distribution and pharmacodynamics. Molecular mechanisms of enhanced release were studied using high-speed centrifugation, molecular dynamics and rheology. The interaction between the CE, MF and skin was studied by tape stripping, CLSM, ATR-FTIR and SAXS. The formulation was optimized to contain 0.05% MF and used 10% polyglyceryl-3 oleate (POCC) as the CE. There was no significant difference from Elocon® cream in in vivo retention and pharmacodynamics but increased in vivo retention by 3.14-fold and in vitro release by 1.77-fold compared to the basic formulation. POCC reduced oil phase cohesive energy density, enhancing drug mobility and release. It disrupted skin lipid phases, aiding drug entry and formed hydrogen bonds, prolonging retention. This study highlights POCC as a CE in the cream, offering insights for semi-solid formulation development.
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  • 文章类型: Journal Article
    目前的工作是构建用于治疗牛皮癣的罗氟司特(ROF)乳膏,并阐明丙二醇单辛酸酯(PGM)在乳膏的分子迁移率中的双重作用。以及通过药物-PGM-神经酰胺和药物-PGM-胶原分子间相互作用的药物-皮肤混溶性。通过稳定性研究和体外皮肤给药研究筛选乳膏配方,Plackett-Burman和Box-Behnken设计进行了优化,最后通过体内组织分布研究进行验证。PGM表现出显著的药物皮肤保留增强作用(体内Rmax=19.5μg/g)。通过减少流变学研究证明的油分子的分子相互作用,增加了乳膏油相的分子迁移率(Ec=3.73×10-4mJ·m-3)。更重要的是,由于良好的角质层(SC)相容性(ΔH=-403.88J/g),PGM促进SC脂质的有序流动(X射线散射,ΔLPP=1.18nm),并大量进入有活力的表皮/真皮(VE/DE)(RPGM=1186μg/g),充当桥梁,通过两个H键将药物连接到胶原蛋白(LengthH键=2.846和3.313),从而显著增加了药物和VE/DE的混溶性(ΔH=-310.10J/g,Emix=21.66千卡/摩尔)。在这项研究中,成功开发了ROF乳膏,并在分子水平上阐明了PGM对皮肤保留的影响。
    The present work was to construct a roflumilast (ROF) cream for the treatment of psoriasis and clarify the dual roles of propylene glycol monocaprylate (PGM) in both molecular mobility of the cream, and drug-skin miscibility via drug-PGM-ceramide and drug-PGM-collagen intermolecular interaction. The cream formulation was screened through the stability study and in vitro skin administration study, optimized by Plackett-Burman and Box-Behnken design, and finally verified by the in vivo tissue distribution study. PGM demonstrated a significant drug skin retention enhancement effect (Rmax in vivo = 19.5 μg/g). It increased the molecular mobility of the oil phase of the cream by decreasing the molecular interaction of oil molecules proven by the rheology study (Ec = 3.73 × 10-4 mJ·m-3). More importantly, because of the good stratum corneum (SC) compatibility (∆H =  - 403.88 J/g), PGM promoted an orderly flow of SC lipids (X-ray scattering, ΔLPP = 1.18 nm) and entered the viable epidermis/dermis (VE/DE) in large quantities (RPGM = 1186 μg/g), acting as a bridge to connect the drug to collagen through two H-bonds (LengthH-bond = 2.846 Å and 3.313 Å), thus increasing the miscibility of drug and VE/DE significantly (∆H =  - 310.10 J/g, Emix = 21.66 kcal/mol). In this study, a ROF cream was developed successfully and the effect of PGM on the skin retention was clarified at molecular level.
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  • 文章类型: Journal Article
    Due to environmental issues caused by plastic packaging and growing consumer demand for fresh and safe food, there is a growing interest in antibacterial active food packaging films/coatings containing plant essential oils (EO). For the effective use of EO-incorporated active films/coatings, EO must be effectively integrated encapsulated in active films/coatings, and the integrated encapsulated EO must be released from active films/coatings slowly during storage to exhibit antibacterial effects more durable. Recently, several promising strategies have been proposed to improve the sustained release and retention enhancement of EO in active films/coatings, including particle encapsulation, nanoemulsion, Pickering emulsions, multilayer system, and electrospinning technology. This article reviewed the latest technologies of sustained release and retention enhancement strategies for encapsulating EO in active films/coatings. The advantages and disadvantages of these sustained release and retention enhancement strategies and their practical applications in food preservation are also introduced.
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