Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars

[Abstract]: Objective: This study evaluates the efficacy of imiquimod liposome gel (IMQ-Lips gel) to prevent and treat hypertrophic scars (HS). Methods: On the basis of an orthogonal L9 (34) design, IMQ-Lips formulations were optimized using the film dispersion-pH gradient method. The optimal param...

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Main Authors: Yujian LIN, Xi LUO, Yanshan ZHAN, Ruiping LIU, Xiaoqi XU, Jun SHI
Format: Article
Language:English
Published: KeAi Communications Co., Ltd. 2021-06-01
Series:Journal of Holistic Integrative Pharmacy
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Online Access:http://www.sciencedirect.com/science/article/pii/S2707368823000158
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author Yujian LIN
Xi LUO
Yanshan ZHAN
Ruiping LIU
Xiaoqi XU
Jun SHI
author_facet Yujian LIN
Xi LUO
Yanshan ZHAN
Ruiping LIU
Xiaoqi XU
Jun SHI
author_sort Yujian LIN
collection DOAJ
description [Abstract]: Objective: This study evaluates the efficacy of imiquimod liposome gel (IMQ-Lips gel) to prevent and treat hypertrophic scars (HS). Methods: On the basis of an orthogonal L9 (34) design, IMQ-Lips formulations were optimized using the film dispersion-pH gradient method. The optimal parameters were phospholipid–cholesterol (3 : 1), lipid-to-drug ratio (8 : 1), and a vitamin E of 5 mg. The in vitro transdermal experiment and rabbit HS model were used to evaluate the pharmacodynamics in vitro and in vivo. Results: IMQ-Lips has good physical and chemical properties, with an encapsulation rate of 81.2% ± 1.9%, an average diameter of (347 ± 21) nm, and a zeta potential of (–12.19 ± 1.7) mV. In vitro transdermal penetration tests showed that IMQ-Lips gel enhanced skin retention and reduced transdermal delivery compared with IMQ gel. The rabbit HS model further revealed that IMQ-Lips gel treatment reduced scar formation by inhibiting overproliferation of fibroblasts and reducing interleukin-4 levels. Conclusion: Taken together, these data suggest that IMQ-Lips gel represents a potential therapeutic approach for HS treatment.
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publisher KeAi Communications Co., Ltd.
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spelling doaj-art-39d7d4cefaaf431f96384c1d6c2298db2025-08-20T02:14:03ZengKeAi Communications Co., Ltd.Journal of Holistic Integrative Pharmacy2707-36882021-06-012212313410.1016/S2707-3688(23)00015-8Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scarsYujian LIN0Xi LUO1Yanshan ZHAN2Ruiping LIU3Xiaoqi XU4Jun SHI5Department of Traditional Chinese Medicine, Guangdong Pharmaceutical University of China, Guangzhou 510006, ChinaDepartment of Traditional Chinese Medicine, Guangdong Pharmaceutical University of China, Guangzhou 510006, ChinaDepartment of Traditional Chinese Medicine, Guangdong Pharmaceutical University of China, Guangzhou 510006, ChinaDepartment of Traditional Chinese Medicine, Guangdong Pharmaceutical University of China, Guangzhou 510006, ChinaDepartment of Traditional Chinese Medicine, Guangdong Pharmaceutical University of China, Guangzhou 510006, ChinaDepartment of Traditional Chinese Medicine, Guangdong Pharmaceutical University of China, Guangzhou 510006, China; Guangdong Local Precision Drug delivery Engineering and Technology Research Center, Guangzhou 510006, China; [Corresponding author][Abstract]: Objective: This study evaluates the efficacy of imiquimod liposome gel (IMQ-Lips gel) to prevent and treat hypertrophic scars (HS). Methods: On the basis of an orthogonal L9 (34) design, IMQ-Lips formulations were optimized using the film dispersion-pH gradient method. The optimal parameters were phospholipid–cholesterol (3 : 1), lipid-to-drug ratio (8 : 1), and a vitamin E of 5 mg. The in vitro transdermal experiment and rabbit HS model were used to evaluate the pharmacodynamics in vitro and in vivo. Results: IMQ-Lips has good physical and chemical properties, with an encapsulation rate of 81.2% ± 1.9%, an average diameter of (347 ± 21) nm, and a zeta potential of (–12.19 ± 1.7) mV. In vitro transdermal penetration tests showed that IMQ-Lips gel enhanced skin retention and reduced transdermal delivery compared with IMQ gel. The rabbit HS model further revealed that IMQ-Lips gel treatment reduced scar formation by inhibiting overproliferation of fibroblasts and reducing interleukin-4 levels. Conclusion: Taken together, these data suggest that IMQ-Lips gel represents a potential therapeutic approach for HS treatment.http://www.sciencedirect.com/science/article/pii/S2707368823000158ImiquimodLiposomesGelHypertrophic scars
spellingShingle Yujian LIN
Xi LUO
Yanshan ZHAN
Ruiping LIU
Xiaoqi XU
Jun SHI
Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars
Journal of Holistic Integrative Pharmacy
Imiquimod
Liposomes
Gel
Hypertrophic scars
title Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars
title_full Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars
title_fullStr Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars
title_full_unstemmed Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars
title_short Imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars
title_sort imiquimod liposome gel preparations and their ability to inhibit hypertrophic scars
topic Imiquimod
Liposomes
Gel
Hypertrophic scars
url http://www.sciencedirect.com/science/article/pii/S2707368823000158
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AT yanshanzhan imiquimodliposomegelpreparationsandtheirabilitytoinhibithypertrophicscars
AT ruipingliu imiquimodliposomegelpreparationsandtheirabilitytoinhibithypertrophicscars
AT xiaoqixu imiquimodliposomegelpreparationsandtheirabilitytoinhibithypertrophicscars
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