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Ethosomes-Silk Fibroin/Polyvinyl Alcohol Composite Hydrogel transdermal drug delivery system : Preparation and Characterization

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Journal of Donghua University(English Edition) 2017年第1期34卷 99-104页

作者：杨兴兴余凡马琳琳骆格杰潘潇涵林思王红声 College of Chemistry Chemical Engineering and Biotechnology Donghua University Shanghai 201620 China Key Laboratory of Textile Science & Technology Ministry of Education Shanghai 201620 China Key Laboratory of Science & Technology of Eco-Textile Ministry of Education Donghua University Shanghai 201620 China

One key of constructing ideal transdermal drug delivery system(TDDS)is enhancing the percutaneous rate of drugs without sacrificing ***(Eths)have excellent transdermal performance as well as good biocompatibility,and thus been widely used as drug *** has good 3-dimensional mesh structure which is convenience for drugs release and *** this study,Eths were introduced into silk fibroin(SF)/polyvinyl alcohol(PVA)composite hydrogel to construct a novel TDDS through a green *** Ethsomes(Eths)-SF/PVA composite hydrogel TDDS showed good mechanical properties(stress:(0.236±0.032)MPa;strain:(65.74±2.45)%).Also,skin fibroblasts can grow and proliferate well on this TDDS,indicating that this material has a good ***,with doxorubicin hydrochloride(Dox)as a model drug loaded in ethosomes,in vitro studies showed that this TDDS was able to transdermally release Dox *** data suggested this novel system had a good potential for application in TDD,though further evaluative study still needed to carry out.

关键词： transdermal drug delivery system Ethosomes(Eths) silk fibroin hydrogel polyvinyl alcohol

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Ionic liquids as the effective technology for enhancing transdermal drug delivery: Design principles, roles, mechanisms, and future challenges

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Asian Journal of Pharmaceutical Sciences 2024年第2期19卷 38-51页

作者： Xuejun Chen Ziqing Li Chunrong Yang Degong Yang Department of Pharmacy Shantou University Medical CollegeShantou 515041China Guangdong Provincial Key Laboratory of Infectious Diseases and Molecular Immunopathology Shantou University Medical CollegeShantou 515041China

Ionic liquids (ILs) have been proven to be an effective technology for enhancing drug transdermal absorption. However, due to the unique structural components of ILs, the design of efficient ILs and elucidation of action mechanisms remain to be explored. In this review, basic design principles of ideal ILs for transdermal drug delivery system (TDDS) are discussed considering melting point, skin permeability, and toxicity, which depend on the molar ratios, types, functional groups of ions and inter-ionic interactions. Secondly, the contributions of ILs to the development of TDDS through different roles are described: as novel skin penetration enhancers for enhancing transdermal absorption of drugs;as novel solvents for improving the solubility of drugs in carriers;as novel active pharmaceutical ingredients (API-ILs) for regulating skin permeability, solubility, release, and pharmacokinetic behaviors of drugs;and as novel polymers for the development of smart medical materials. Moreover, diverse action mechanisms, mainly including the interactions among ILs, drugs, polymers, and skin components, are summarized. Finally, future challenges related to ILs are discussed, including underlying quantitative structure-activity relationships, complex interaction forces between anions, drugs, polymers and skin microenvironment, long-term stability, and in vivo safety issues. In summary, this article will promote the development of TDDS based on ILs.

关键词： transdermal drug delivery system Ionic liquid Quantitative structure-activity relationship Intermolecular interaction

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Microneedles for Enhanced Topical Treatment of Skin Disorders:Applications,Challenges,and Prospects

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Engineering 2023年第11期30卷 170-189页

作者： Tingting Peng Yangyan Chen Wanshan Hu Yao Huang Minmin Zhang Chao Lu Xin Pan Chuanbin Wu International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative drug Development Ministry of Education of the People’s Republic of ChinaCollege of PharmacyJinan UniversityGuangzhou 511436China School of Pharmaceutical Sciences Sun Yat-sen UniversityGuangzhou 510006China Faculty of Pharmacy University of HelsinkiHelsinki 00014Finland

Microneedles(MNs)can be used for the topical treatment of skin disorders as they directly deliver therapeutics to the site of skin lesions,resulting in increased therapeutic efficacy while having minimum side *** are used to deliver different kinds of therapeutics(e.g.,small molecules,macromolecules,nanomedicines,living cells,bacteria,and exosomes)for treating various skin disorders,including superficial tumors,wounds,skin infections,inflammatory skin diseases,and abnormal skin *** therapeutic efficacy of MNs can be improved by integrating the advantages of multiple therapeutics to perform combination *** careful designing,MNs can be further modified with biomimetic structures for the responsive drug release from internal and external stimuli and to enhance the transdermal delivery efficiency for robust therapeutic *** studies have proposed the use of drug-free MNs as a promising mechanotherapeutic strategy to promote wound healing,scar removal,and hair regeneration via a mechanical communication *** MNs have several advantages,the practical application of MNs suffers from problems related to industrial manufacture and clinical evaluation,making it difficult for clinical *** this study,we summarized the various applications,emerging challenges,and developmental prospects of MNs in skin disorders to provide information on ways to advance clinical translation.

关键词： Microneedles transdermal drug delivery system Skin disorders Treatments Challenges Prospects

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The enhancing effect and promoting mechanisms of the stereoisomeric monoterpene alcohol esters as enhancers for drugs with different physicochemical properties

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Asian Journal of Pharmaceutical Sciences 2022年第1期17卷 139-152页

作者： Heping Wang Yan Li Chunyan Wang Jing Wang Bo Ren Xiaona Li Mingzhu Li Dandan Geng Chensi Wu Ligang Zhao School of Pharmacy North China University of Science and TechnologyTangshan 063000China Dept of Pharmacy Tangshan Maternal and Child Health HospitalTangshan 063000China Tangshan key laboratory of novel preparations and drug release technology Tangshan 063000China

To explore the structure-activity connections of amphiphilic permeation enhancers containing the length of the hydrophobic chains as well as the properties of the polar head,O-acylgeraniol and O-acylnerol derivatives were synthesized from geraniol/nerol(cis-isomer of geraniol) and pharmaceutical excipient acids in this research. Their promotion of the percutaneous absorption of three drugs as the model, flurbiprofen(FP), isosorbide dinitrate(ISDN) and donepezil(DNP), which were selected based on their physicochemical properties,was tested by in vitro skin penetration and in vivo. Molecular simulation, ATR-FTIR, CLSM and histological observation were implement to evaluate the mode of action of the *** results indicated that(E)-3,7-dimethyl-2,6-octadien-1-yl tetradecanoate(GER-C14, trans-)achieved the highest enhancement ability for the three drugs;additionally, the in vivo results obtained were in good correlation with the in vitro data. Molecular docking results suggested that enhancers loosen the hydrogen bonds between ceramides, and the results of molecular simulation indicated that GER-C14, NER-C14 could insert into the middle of the lipid bilayer to form an independent phase. According to ATR-FTIR and histological evaluation, the enhancers extracted lipids and influenced the protein region, thereby disturbing the skin array. In addition, CLSM described the dynamic effects of enhancers on lipids between stratum corneum(SC) cells. In conclusion, GER-C14 had a better penetration promotion effect, which broadened our understanding of stereoisomeric penetration enhancers.

关键词： O-acylgeraniol derivatives O-acylnerol derivatives transdermal drug delivery system In vitro and in vivo correlation Enhancing mechanism

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Nano-formulations for transdermal drug delivery:A review

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Chinese Chemical Letters 2018年第12期29卷 1713-1724页

作者： Xingli Zhou Ying Hao Liping Yuan Sushmita Pradhan Krista Shrestha Ojaswi Pradhan Hongjie Liu Wei Li Department of Dermatovenereology State Key Laboratory of BiotherapyWest China HospitalSichuan University

transdermal drug delivery refers to a means of delivering drugs through the surface of the skin for local or systemic treatment. The drug functions after absorption through the skin into the systemic circulation via capillary action at a certain rate. Use of traditional physical and chemical enhancers to improve the transdermal permeation rate by increasing drug solubility, diffusion coefficient, and reservoir effect is not feasible owing to the toxic side effects of the overuse of chemical penetration enhancers. Nanoformulations generally vary in size and range from 10 nm to 100 nm. The smaller particle size leads to increased drug permeability, stability, retention, and targeting, making nano-formulations suitable for transdermal drug delivery. The different applications of nano-formulations(vesicles or nanoparticles and nanoemulsions) have been widely studied. Here, the classification, characteristics, transdermal mechanism, and application of the most popular nano-formulations in transdermal drug delivery system are reviewed.

关键词： Nano-formulation transdermal drug delivery system Classification Mechanism Application

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Combination of hydroxypropyl-β-cyclodextrin with nanoemulsion for enhancing resveratrol percutaneous delivery and treatment in skin photoaging

Combination of hydroxypropyl-β-cyclodextrin with nanoemulsi...

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2018年第十二届中国药物制剂大会

作者：曹思思 Yueming Long Yixuan Wang Kaiyue Yu Yuanhao Zhai Yuehong Xu School of Pharmaceutical Sciences Sun Yat-sen University

Repeated UV exposure can cause cutaneous oxidative stress and inflammation, resulting in premature skin photoaging, and even skin cancer. Resveratrol（RES） has arisen increasing attention due to its antioxidant and anti-inflammatory properties in addition to its amicable safety profile. However, the shortcomings such as its poor solubility, chemical instability, and low oral bioavailability have limited its application. This study was to prepare a hydroxypropyl-β-cyclodextrin（HP-β-CD） combined with nanoemulsion（NE） formulation to encapsulate resveratrol（RES-CD-NE）, increasing the solubility and the stability of resveratrol. RES-CD-NE consisted of oil phase（Labrafil M 1994 CS）, surfactant and co-surfactant（Solutol HS15 and Transcutol P）, 15%（w/w） HP-β-CD solution and 1%（w/w） RES. 1 H NMR spectra strongly confirmed the inclusion complex formation of RES and HP-β-CD. RES was encapsulated effectively and the stability was improved, resulting in the excellent transdermal efficiency both in vitro and in vivo skin permeation studies. The cell experiment verified that RES-CD-NE had higher cellular uptake efficiency, thus reducing the level of ROS and enhancing skin permeation. The wrinkles, roughness, dryness and laxity caused by photoaging were prevented and the activity of antioxidant enzymes superoxide dismutase（SOD） in the skin was improved after RES-CD-NE treatment. In conclusion, HP-β-CD combined with NE could encapsulate resveratrol effectively. The solubility and the stability of RES were improved. RES-CD-NE showed a promising prospect in photoaging treatment.

关键词： Resveratrol nanoemulsion hydroxypropyl-β-cyclodextrin transdermal drug delivery system photoaging

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