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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2023 · IF 5

The preparation of high minoxidil loaded transfersomes and its gel for effective topical treatment of alopecia

Ying Sun,Yongxiang Zhang,Xiaxia Liu,Yan Tingting,Liyan Shen,Dan Ye,Xia Kong,Yonghui Su,Qingping Tian

Transfersomes is one of the most effective nanotechnology-based formulation for transdermal delivery of minoxidil (MXD), however the potential use was limited by its low drug content ( DC ) and entrapment efficiency ( EE ). In this study, efforts have been made to improve DC and EE of MXD in transfersomes for effective topical treatment of alopecia . By dissolving both MXD and edge activator (Tween 80) in aqueous phase than either or both of them co-dissolving in organic solvent with lipids (phospholipid and cholesterol with mass ratio of 5:1), the DC and EE of MXD transfersomes prepared by thin film hydration method were significantly increased. The optimized transfersomes (MT) and its gel (MT gel ) with mass ratio of drug, Tween 80 and lipids 3:1:18 have a spherical morphology without aggregation, and a particle size of not more than 100 nm. The differential scanning calorimetry measurements revealed that the drug in MT was in the non-crystalline state. MT and MT gel exhibited better in vitro transdermal penetration ability and hair of C57BL/6 mice growth-promoting capacity than commercial formulations. MT gel has non-irritation and is better than MT in skin adhesion, stability, potential for skin storage and hair growth promotion ability, which could endow it to be a promising strategy for topical treatment of alopecia.

CAS / MDL: 69-65-8
研究领域: 药剂学 · 纳米技术 · 皮肤科学
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Drug Delivery and Translational Research · 2025 · IF 5.5

Minoxidil cyclodextrin inclusion complex-loaded microemulsions and transfersomes for androgen alopecia treatment: a comparative study

Zhang Min,Pang Xiaoya,Kang Shuhui,Sui Hao,Kong Xia,Wang Gang,Wang Ruixuan,Shen Guiqing,Tian Qingping

Our MXD/SCD@TF designed by the combination of transfersome and inclusion technology was obviously superior to commercial 2% MXD tincture in treating androgenetic alopecia (AGA) in mice, but its complex preparation and poor stability undoubtedly increased both development and usage costs. In this paper, using our previous alcohol-free low surfactant microemulsion technology with VES as auxiliary oil phase, microemulsions loaded with the inclusion complex of MXD and sulfobutylether-β-cyclodextrin (SBE-β-CD) were prepared, optimized and characterized, and the therapeutic effect on AGA C57BL/6 mice was compared with MXD/SCD@TF. According to the ternary phase diagram, steady-state permeation rate of MXD through SD rat skin and drug retention, MXD/SCD@ME was selected as the optimal prescription, composed of 5.25% oil phase, 9.75% surfactants, 10.20% SBE-β-CD, 1.02% MXD and 73.78% water, which conformed to the characteristics of microemulsion. MXD/SCD@ME had good stability, and the application of inclusion technology increased the MXD loading in microemulsion to nearly 5 times. The results of in vivo skin penetration test and laser confocal scanning visualization showed that MXD/SCD@ME was easier to deliver drugs to deeper skin tissues than MXD/SCD@TF. Hair regeneration study demonstrated that MXD/SCD@ME had higher ability than MXD/SCD@TF in promoting hair growth, prolonging hair growth period, reducing ROS level and promoting cell proliferation of hair follicles. In addition, the blank microemulsion of MXD/SCD@ME had certain therapeutic effect on AGA, indicating the synergistic effect between VES and MXD. All these indicated that MXD/SCD@ME is expected to provide a better choice for pharmacological therapy of MXD on AGA than MXD/SCD@TF. Graphical

CAS / MDL: 3326-32-7
研究领域: 药剂学 · 皮肤科学 · 生物医学工程
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CHIRALITY · 2019 ·Vol. 32 ·期 1 ·98-106 · IF 1.927

A rapid enantioseparation system of capillary electrochromatography modified by electrostatic adsorption with transfersomes

Zhifeng Huang,Yingxiang Du,Xiaoqi Li,Zijie Feng,Xiaodong Sun,Xiaofei Ma,Mingxuan Ma

Transfersomes were a special kind of nanomaterials with higher deformability and flexibility. A rapid method for coated-column preparation using anionic transfersomes as a coating material by electrostatic adsorption was developed. With carboxymethyl-β-cyclodextrin added in running buffer as the chiral selector, the capillary electrochromatography enantioseparation system based on the transfersomes-coated column modified by electrostatic adsorption was established for the first time. Propranolol and metoprolol acted as model drugs to evaluate the enantioseparation performance, these two basic drugs achieved baseline separation with satisfactory resolution and selection factor in this transfersomes-electrochromatography system but only partial separation in bare column system. In order to get the optimal separation condition, concentration of chiral selector, buffer pH, and applied voltage were systematically investigated. A rapid and efficient enantioseparation electrochromatography system was established and showed that transfersomes as the stationary phase could efficiently improve chiral separation effect.

CAS / MDL: 97281-47-5 26062-79-3
研究领域: 分析化学 · 药学 · 纳米技术
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Separation Science Plus · 2019 ·Vol. 2 ·期 5 ·178-185 · IF 0

Enantioseparation of basic drugs by capillary electrochromatography using a stationary phase of transfersomes

Zhifeng Huang,Yingxiang Du,Xiaoqi Li,Xiaodong Sun,Zijie Feng,Xiaofei Ma

Transfersomes, a special kind of phospholipid vesicles with higher deformability and flexibility, were applied as coating material to prepare a transfersomes-coated capillary column. A capillary electrochromatography enantioseparation system based on the new transfersomes-coated column with carboxymethyl-β-cyclodextrin added to the running buffer as a chiral selector was established for the first time. Compared with a bare column, three basic drugs achieved baseline separation with better resolution (3.17 for Propranolol, 2.38 for Metoprolol, 2.34 for Esmolol) in this transfersomes-electrochromatography system. Several important parameters including concentration of chiral selector, buffer pH and applied voltage were systematically investigated to provide the optimal separation condition. This study constructed a flexible and efficient enantioseparation electrochromatography system with a small amount of transfersomes, and showed that transfersomes as the stationary phase could efficiently improve chiral separation effect.

研究领域: 分析化学 · 药学 · 色谱学
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