Liposomes Carrying Diclofenac Diethylammonium: A Penetrability and Permeation Study  

作　　者：Adriana Camino Anyoli Taly Cirana Rodriguez Alfredo Inatti Evelyn Pena Xenon Serrano Adriana Camino;Anyoli Taly;Cirana Rodriguez;Alfredo Inatti;Evelyn Pena;Xenon Serrano(Department of R & D, Nanotechnology Laboratory, Industrias Biocontrolled, Grupo Leti, S.A.V., Guarenas, Venezuela;Department of Clinical Research, Industrias Biocontrolled, Grupo Leti, S.A.V., Guarenas, Venezuela)

机构地区：[1]Department of R & D, Nanotechnology Laboratory, Industrias Biocontrolled, Grupo Leti, S.A.V., Guarenas, Venezuela [2]Department of Clinical Research, Industrias Biocontrolled, Grupo Leti, S.A.V., Guarenas, Venezuela

出　　处：《Journal of Biosciences and Medicines》2024年第12期206-218,共13页生物科学与医学(英文)

摘　　要：This study investigated whether liposomes could enhance the permeation and penetration of diclofenac diethylammonium. For this, a 1.16% diclofenac diethylammonium liposome gel formulation was developed (Grupo Leti, S.A.V.). In vitro and ex vivo tests were conducted to analyze the diffusion and penetration profiles of the formulation. The profiles obtained were compared with a commercially available product, DiAnalper gel (Pharmetique Labs). The in vitro test was assessed in a Franz diffusion cell system using a dialysis membrane. The cumulative amount of drug permeated after 24 h demonstrated a significantly (p 2, whereas the commercial formulation yielded values of 371.00 ± 3.54 μg/cm2. These findings were further supported by consistent results in the percentage of drug release, flux, and permeability coefficient, all indicating a notable improvement in diffusion associated with the liposomal gel formulation. The tape stripping assay performed on pig ear skin demonstrates a statistically significant difference (p < 0.05) between the penetration transport of the diclofenac from liposome gel formulation (1413.95 ± 250.51 μg) and the conventional product (202.36 ± 18.07 μg) the liposomal formulation was able to cross de stratum corneum and deliver a high amount of drug to the skin. These findings demonstrated that incorporating diclofenac into a liposomal system significantly improved the drug delivery, which could confer an advantage for clinical uses.This study investigated whether liposomes could enhance the permeation and penetration of diclofenac diethylammonium. For this, a 1.16% diclofenac diethylammonium liposome gel formulation was developed (Grupo Leti, S.A.V.). In vitro and ex vivo tests were conducted to analyze the diffusion and penetration profiles of the formulation. The profiles obtained were compared with a commercially available product, DiAnalper gel (Pharmetique Labs). The in vitro test was assessed in a Franz diffusion cell system using a dialysis membrane. The cumulative amount of drug permeated after 24 h demonstrated a significantly (p 2, whereas the commercial formulation yielded values of 371.00 ± 3.54 μg/cm2. These findings were further supported by consistent results in the percentage of drug release, flux, and permeability coefficient, all indicating a notable improvement in diffusion associated with the liposomal gel formulation. The tape stripping assay performed on pig ear skin demonstrates a statistically significant difference (p < 0.05) between the penetration transport of the diclofenac from liposome gel formulation (1413.95 ± 250.51 μg) and the conventional product (202.36 ± 18.07 μg) the liposomal formulation was able to cross de stratum corneum and deliver a high amount of drug to the skin. These findings demonstrated that incorporating diclofenac into a liposomal system significantly improved the drug delivery, which could confer an advantage for clinical uses.

关 键 词：Liposomes Diclofenac Diethylammonium Transdermal Drug Delivery Skin Permeation Skin Penetration 

分 类 号：R96[医药卫生—药理学]