不同剂型8-甲氧基补骨脂素柔性纳米脂质体的大鼠体外透皮研究

目的:对8-甲氧基补骨脂素(8-MOP)柔性纳米脂质体凝胶、8-MOP柔性纳米脂质体、8-MOP酊剂三种剂型药物的透皮差异进行比较,探讨三种不同剂型8-甲氧基补骨脂素柔性纳米脂质体的大鼠体外透皮性。方法:将三种不同剂型8-MOP通过含有离体鼠皮的扩散池,测定鼠皮以及接受池中8-MOP的含量,并进行比较,对不同时间点3种不同剂型8-MOP的累积渗透量作图,对各组皮肤滞留量两两进行t检验。结果:8-MOP脂质体凝胶组在接受液中的累积渗透量小于8-MOP脂质体组和酊剂组;8-MOP酊剂组渗透量从第3 h后开始急剧升高;比较各组皮肤内滞留的药量,8-MOP脂质体凝胶组高于8-MOP酊剂组,而8-MOP脂质体组又高于MOP脂质体凝胶组,差异均有统计学意义(t值分别为53.97、18.97,P值均<0.05)。结论:8-MOP不同剂型有着不同的特性,8-MOP柔性纳米脂质体更具有皮肤亲和性,更有利于药物在皮肤内滞留发挥药物作用。     

不同剂型8-甲氧基补骨脂素柔性纳米脂质体的大鼠体外透皮研究

目的:对8-甲氧基补骨脂素(8-MOP)柔性纳米脂质体凝胶、8-MOP柔性纳米脂质体、8-MOP酊剂三种剂型药物的透皮差异进行比较,探讨三种不同剂型8-甲氧基补骨脂素柔性纳米脂质体的大鼠体外透皮性。方法:将三种不同剂型8-MOP通过含有离体鼠皮的扩散池,测定鼠皮以及接受池中8-MOP的含量,并进行比较,对不同时间点3种不同剂型8-MOP的累积渗透量作图,对各组皮肤滞留量两两进行t检验。结果:8-MOP脂质体凝胶组在接受液中的累积渗透量小于8-MOP脂质体组和酊剂组;8-MOP酊剂组渗透量从第3 h后开始急剧升高;比较各组皮肤内滞留的药量,8-MOP脂质体凝胶组高于8-MOP酊剂组,而8-MOP脂质体组又高于MOP脂质体凝胶组,差异均有统计学意义(t值分别为53.97、18.97,P值均0.05)。结论:8-MOP不同剂型有着不同的特性,8-MOP柔性纳米脂质体更具有皮肤亲和性,更有利于药物在皮肤内滞留发挥药物作用。     

8-甲氧基补骨脂素柔性纳米脂质体的制备工艺

目的:优选8-甲氧基补骨脂素(8-methoxypsoralan,8-MOP)柔性纳米脂质体的制备工艺条件。方法:通过正交设计优选该脂质体的处方及制备工艺,用扫描电镜观测其外观及分布,采用高速离心法处理样品,测定其包封率。结果:所得脂质体外观圆整,分布较均匀,平均包封率(89.7±1.2)%(n=5)。结论:该脂质体制备工艺可行,具有开发价值。     

表没食子儿茶素没食子酸酯-补骨脂脂质体的制备及体外透皮性质研究

目的：制备表没食子儿茶素没食子酸酯-补骨脂脂质体（EGCG-PL）并检测其体外透皮性。方法：采用逆向蒸发法制备EGCG-PL，以激光粒度仪测定EGCG-PL的粒度及Zeta电位，超滤-HPLC法测定包封率，Franz 扩散装置比较EGCG-PL与EGCG-补骨脂醇溶液组（EGCG-PS）体外透皮性质的差异。结果：所制备的EGCG-PL粒径分布均匀，平均粒径为(118.1±17.0)nm，Zeta电位为-29.3 mV。EGCG-PL中EGCG、补骨脂素及异补骨脂素的包封率分别为(85.58±1.07)%、(55.49±2.82)%和(53.73±1.29)%。体外透皮试验结果显示，EGCG-PL中EGCG、补骨脂素及异补骨脂素24 h单位面积累积透过量及皮肤滞留量均明显高于EGCG-PS。结论：EGCG-PL制备简便、质量稳定。     

茶多酚二元醇脂质体的制备及质量评价

目的: 制备茶多酚二元醇脂质体（TP-EL）并对其质量进行评价。方法: 以包封率作为评价指标进行正交试验筛选最佳处方及制备工艺,并评价二元醇脂质体的质量。结果: 各因素最佳的水平组合为：磷脂浓度为4%、磷脂与胆固醇的比为5:1、药脂比为1:8、搅拌时间为40 min。所制备的脂质体大多数为单室脂质体,平均粒径为 123.0 ± 13.2 nm,多分散性指数(PDI)为 0.15 ± 0.07。TP-EL的Zeta 电位为 -35.2 mV,且包封率达71.82 ± 2.03%。结论: 该制剂制备简便、质量稳定。     

表没食子儿茶素没食子酸酯明胶纳米粒的制备及体外透皮性质研究

目的：制备表没食子儿茶素没食子酸酯-明胶纳米粒(EGCG-N)并研究其体外透皮性。方法：以激光粒度仪测定EGCG-N的粒度及Zeta电位,超滤-HPLC法测定EGCG-N的载药量及包封率,Franz扩散装置检测EGCG-N体外透皮性。结果：所制备的EGCG-N粒径分布均匀,平均粒径为(72.63±0.47)nm,Zeta电位为-28.0mV。EGCG-N中EGCG的载药量和包封率分别为(29.82±2.16)%和(83.91±0.93)%。EGCG-N中EGCG 24 h单位面积累积透过量及皮肤滞留量分别为(133.77±22.79)μg/cm²和(492.57±37.68)μg/g均明显高于EGCG溶液剂(53.30±21.12)μg/cm²和(165.88±17.96)μg/g(均P<0.01)。结论：EGCG-N制备简便,能够提高EGCG的经皮渗透能力。     

0.5%鬼臼毒素纳米脂质载体的制备及理化性质考察

目的：纳米脂质载体（nanostructured lipid carrier,NLC）具有较高的载药量和物理稳定性。为提高鬼臼毒素（podophyllotoxin,POD）的治疗效果,降低毒副作用,本研究探讨了POD浓度为5 g/L（0.5%）的POD-NLC的制备方法及理化性质。方法：POD-NLC的制备采用乳化蒸发-低温固化法,设计正交实验优化POD-NLC的制备工艺及配方,用透射电镜、粒径仪、高效液相色谱法、pH计考察POD-NLC理化性质。结果：POD-NLC基本呈球状或椭球形,平均粒径（180±20）nm,多分散指数为0.165,pH值为6.20±0.04,包封率为（82.9±2）%。结论：成功制得了POD浓度为5 g/L（0.5%）的POD-NLC,其制备工艺简单,粒径分布较均匀,包封率高,稳定性较好。     

pVAX-Hsp70-HSV2gD DNA疫苗阳离子脂质体的制备

目的制备pVAX-Hsp70-HSV2gD DNA疫苗阳离子脂质体,为基因免疫和基因治疗寻找一种简单、经济、有效的DNA投递系统。方法采用逆向蒸发法,用卵磷脂、胆固醇、十八胺制备成阳离子脂质体包封pVAX-Hsp70-HSV2gD DNA疫苗,在透射电镜下观察脂质体颗粒的大小,应用紫外分光光度计检测DNA疫苗的包封率,免疫组化检测其转染真核细胞的效果。结果制备的脂质体呈圆形、粒径大小较一致,平均粒径为580nm,DNA疫苗脂质体包封率达到50%~55%,能有效转染真核细胞。结论成功制备了pVAX-Hsp70-HSV2gD DNA疫苗阳离子脂质体。该方法作为提高基因免疫效果的简单、经济、有效的手段之一,为其进一步的研究打下了基础。     

人源性抗角蛋白Fab抗体脂质体的制备

目的制备人源性抗角蛋白Fab抗体(HAKFA)脂质体,检测脂质体的体外释放及包裹和游离抗体的活性,探索HAKFA可行的应用途径。方法采用逆相蒸发与钙融合联合法制备HAKFA脂质体,在透射电镜下观察脂质体颗粒的性状及大小,应用紫外分光光度计检测抗体的包封率,ELISA检测包裹前后的抗体活性。结果本方法制备的脂质体呈现圆形、粒径大小较一致,约50~100nm;HAKFA脂质体包封率达到(60.3±12.7)%;HAKFA脂质体呈现缓释特性并且抗体依然保持良好的抗原结合活性。结论逆相蒸发与钙融合法为制备HAKFA脂质体较理想的方法。     

0.5%鬼臼毒素纳米脂质载体包封率的测定

目的：建立新的测定鬼臼毒素纳米脂质载体包封率的高效液相色谱法。方法：以ODS-C18（4.6 mm×250 mm5,μm）为分析柱,以甲醇-0.6%冰醋酸（52∶48）为流动相,流速1 mL.min-1,检测紫外线波长为291 nm,进样量20μL,柱温40℃。采用4℃12 000 r/min离心30分钟分离脂质体和游离药物,测定包封率。结果：当鬼臼毒素浓度在0.5～200μg/mL范围内时,峰面积与浓度之间呈良好的线性关系（r=0.999 1,n=8）,高、中、低3个剂量的回收率分别为98.6%,96.98%,98.6%,日内精密度0.735%3,批鬼臼毒素纳米脂质载体中鬼臼毒素的包封率分别为84.9%、80.9%8、3.0%。结论：高速离心-HPLC法适合测定0.5%鬼臼毒素纳米脂质载体中鬼臼毒素的包封率。     

Formulation,optimization, and in vitro evaluation of nanostructured lipid carriers for topical delivery of Apremilast

This work was aimed to formulate topical Apremilast (APM)‐loaded nanostructured lipid carriers (NLCs) for the management of psoriasis. NLCs were prepared by a cold homogenization technique using Compritol 888ATO, oleic acid, Tween 80 and Span 20, and Transcutol P as a solid lipid, liquid lipid, surfactant mixture, and penetration enhancer, respectively. Carbopol 940 was used to convert NLC dispersion into NLC‐based hydrogel to improve its viscosity for topical administration. The optimized formulation was characterized for size, polydispersity index (PDI), zeta potential (ZP), percentage of entrapment efficiency (%EE), and surface morphology. Furthermore, viscosity, spreadability, stability, in vitro drug diffusion, ex vivo skin permeation, and skin deposition studies were carried out. APM‐loaded NLCs showed a narrow PDI (0.339) with a particle size of 758 nm, a %EE of 85.5%, and a ZP of −33.3 mV. Scanning electron microscopy confirmed spherical shape of NLCs. in vitro drug diffusion and ex vivo skin permeation results showed low drug diffusion, sustained drug release, and 60.1% skin deposition. The present study confirms the potential of the nanostructured lipid form of poorly water‐soluble drugs for topical application and increased drug deposition in the skin.     

Barium sulphate with a negative zeta potential accelerates skin permeability barrier recovery and prevents epidermal hyperplasia induced by barrier disruption

BACKGROUND: Barium sulphate, a stable inorganic material, has been used in contrast media and cosmetic products because of its stability. As a negative external electric potential accelerates the skin barrier repair after barrier disruption, we hypothesized that topical application of barium sulphate may affect the skin barrier recovery rate depending on its zeta potential. OBJECTIVES: To investigate whether barium sulphate particles in aqueous solution have different zeta potentials depending on their surface structure, and to investigate the possible relation between zeta potential and skin barrier recovery rate. METHODS: Mice were subjected to tape stripping to disrupt barrier function, or were treated with acetone and kept in a dry environment to induce epidermal hyperplasia. They were then treated with different forms of barium sulphate, and barrier recovery was monitored by measurements of transepidermal water loss. RESULTS: There was a significant correlation between the barrier recovery rate and zeta potential of barium sulphate applied topically. Barium sulphate with a negative zeta potential significantly accelerated barrier recovery, but barium sulphate with a positive zeta potential did not accelerate or even delayed barrier repair. Barium sulphate with a negative zeta potential had an X-ray diffraction pattern different from that with a positive potential. The distribution of calcium in the epidermis was also influenced by the polarity of zeta potential. CONCLUSIONS: These findings suggest a new pharmacological approach towards altering barrier function or epidermal hyperplasia with inorganic particles in healthy and diseased skin.     

Formulation and evaluation of carrot seed oil-based cosmetic emulsions

The present study deals with the evaluation of antiaging potential of carrot seed oil-based cosmetic emulsions. Briefly, cosmetic emulsions composed of carrot seed oil in varying proportions (2, 4, and 6% w/v) were prepared using the hydrophile–lipophile balance (HLB) technique. Coconut oil, nonionic surfactants (Tween 80 and Span 80), and xanthan gum were used as the oil phase, emulgent, and emulsion stabilizer, respectively. The formed emulsions were evaluated for various physical, chemical, and biochemical parameters such as the zeta potential, globule size measurement, antioxidant activity, sun protection factor (SPF), skin irritation, and biochemical studies. The zeta potential values ranged from ?43.2 to ?48.3, indicating good stability. The polydispersity index (PDI) of various emulsion formulations ranged from 0.353 to 0.816. 1,1-Diphenyl-2-picrylhydrazyl- (DPPH) and nitric oxide-free radical scavenging activity showed the antioxidant potential of the prepared carrot seed oil emulsions. The highest SPF value (6.92) was shown by F3 having 6%w/v carrot seed oil. Histopathological data and biochemical analysis (ascorbic acid (ASC) and total protein content) suggest that these cosmetic emulsions have sufficient potential to be used as potential skin rejuvenating preparations.     

The effects of photosensitizers and ultraviolet irradiation on the biosynthesis and metabolism of prostaglandins

Prostaglandin biosynthesis from arachidonic acid by skin microsomal fraction preparation was enhanced by UV～irradiation at wavelengths of 254 and 360 nm. In the presence of S-methoxy psoralen (8 MOP) and coal tar, prostaglandin biosynthesis was further enhanced approximately 2-fold by UV-irradiation at 254 nm. Stimulation was less by UV-irradiation at 360 nm. 8-MOP enhanced the conversion of PGE, into PGF_2α by PGE₂-9-ketoreductase prepared from skin high speed supernatant fractions. UV-irradiation at 254 nm and 360 nm with or without the photosensitizers had no effect on the activity of the PGE₂-9-ketoreductase. These data therefore indicate that the action of UV-irradiation, 8-methoxy psoralen and coal tar on the skin may in part be due to their regulation of the biosynthesis and metabohsm of prosta-glandins in this tissue.     

Meshed split skin graft for extensive vitiligo

A 30 year old female presented with generalized stable vitiligo involving large areas of the body. Since large areas were to be treated it was decided to do meshed split skin graft. A phototoxic blister over recipient site was induced by applying 8 MOP solution followed by exposure to UVA. The split skin graft was harvested from donor area by Padgett dermatome which was meshed by an ampligreffe to increase the size of the graft by 4 times. Significant pigmentation of the depigmented skin was seen after 5 months. This procedure helps to cover large recipient areas, when pigmented donor skin is limited with minimal risk of scarring. Phototoxic blister enables easy separation of epidermis thus saving time required for dermabrasion from recipient site.