Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation

Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation

Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loa...

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Main Authors: Mahmood, Syed, Mandal, Uttam K., Chatterjee, Bappaditya
Format: Article
Language:English
English
Published: Elsevier B.V. 2018
Subjects:
RS Pharmacy and materia medica
Online Access:http://umpir.ump.edu.my/id/eprint/20675/
http://umpir.ump.edu.my/id/eprint/20675/
http://umpir.ump.edu.my/id/eprint/20675/
http://umpir.ump.edu.my/id/eprint/20675/1/Transdermal%20delivery%20of%20raloxifene%20HCl%20via%20ethosomal%20system_%20Formulation%2C%20advanced%20characterizations%20and%20pharmacokinetic%20evaluation.pdf
http://umpir.ump.edu.my/id/eprint/20675/7/Transdermal%20delivery%20of%20raloxifene%20HCl%20via%20ethosomal%20system.%20Formulation%2Cadvanced%20characterizations%20and%20pharmacokinetic%20evaluation.pdf
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spelling ump-206752018-08-06T03:36:25Z http://umpir.ump.edu.my/id/eprint/20675/ Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation Mahmood, Syed Mandal, Uttam K. Chatterjee, Bappaditya RS Pharmacy and materia medica Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method. The prepared systems were characterised by high resolution transmission electron microscopy (HRTEM), force emission electron microscopy (FESEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and 31P-NMR study. All these advanced characterization study established that the ethosome formulation was well defined by its size, shape and its bilayer formation. Transdermal flux of the optimized ethosome formulation was 22.14±0.83µg/ml/cm2 which was 21 times higher when compared to the conventional liposomes. Confocal microscopy study revealed an enhanced permeation of coumarin-6 dye loaded ethosomes to much deeper layers of skin when compared with conventional liposomes. The gel was found to be pseudoplastic with elastic behaviour.In-vivo studies on rats showed a higher bioavailability of RXL (157% times) for ethosomal formulation when compared with the oral formulation. In conclusion, RXL loaded ethosomal formulation via transdermal route showed superior drug delivery properties as compared to oral formulation. Elsevier B.V. 2018-05 Article PeerReviewed pdf en http://umpir.ump.edu.my/id/eprint/20675/1/Transdermal%20delivery%20of%20raloxifene%20HCl%20via%20ethosomal%20system_%20Formulation%2C%20advanced%20characterizations%20and%20pharmacokinetic%20evaluation.pdf pdf en http://umpir.ump.edu.my/id/eprint/20675/7/Transdermal%20delivery%20of%20raloxifene%20HCl%20via%20ethosomal%20system.%20Formulation%2Cadvanced%20characterizations%20and%20pharmacokinetic%20evaluation.pdf Mahmood, Syed and Mandal, Uttam K. and Chatterjee, Bappaditya (2018) Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation. International Journal of Pharmaceutics, 542 (1-2). pp. 36-46. ISSN 0378-5173 https://doi.org/10.1016/j.ijpharm.2018.02.044 10.1016/j.ijpharm.2018.02.044
repository_type Digital Repository
institution_category Local University
institution Universiti Malaysia Pahang
building UMP Institutional Repository
collection Online Access
language English
English
topic RS Pharmacy and materia medica
spellingShingle RS Pharmacy and materia medica
Mahmood, Syed
Mandal, Uttam K.
Chatterjee, Bappaditya
Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation
description Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method. The prepared systems were characterised by high resolution transmission electron microscopy (HRTEM), force emission electron microscopy (FESEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and 31P-NMR study. All these advanced characterization study established that the ethosome formulation was well defined by its size, shape and its bilayer formation. Transdermal flux of the optimized ethosome formulation was 22.14±0.83µg/ml/cm2 which was 21 times higher when compared to the conventional liposomes. Confocal microscopy study revealed an enhanced permeation of coumarin-6 dye loaded ethosomes to much deeper layers of skin when compared with conventional liposomes. The gel was found to be pseudoplastic with elastic behaviour.In-vivo studies on rats showed a higher bioavailability of RXL (157% times) for ethosomal formulation when compared with the oral formulation. In conclusion, RXL loaded ethosomal formulation via transdermal route showed superior drug delivery properties as compared to oral formulation.
format Article
author Mahmood, Syed
Mandal, Uttam K.
Chatterjee, Bappaditya
author_facet Mahmood, Syed
Mandal, Uttam K.
Chatterjee, Bappaditya
author_sort Mahmood, Syed
title Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation
title_short Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation
title_full Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation
title_fullStr Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation
title_full_unstemmed Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation
title_sort transdermal delivery of raloxifene hcl via ethosomal system: formulation, advanced characterizations and pharmacokinetic evaluation
publisher Elsevier B.V.
publishDate 2018
url http://umpir.ump.edu.my/id/eprint/20675/
http://umpir.ump.edu.my/id/eprint/20675/
http://umpir.ump.edu.my/id/eprint/20675/
http://umpir.ump.edu.my/id/eprint/20675/1/Transdermal%20delivery%20of%20raloxifene%20HCl%20via%20ethosomal%20system_%20Formulation%2C%20advanced%20characterizations%20and%20pharmacokinetic%20evaluation.pdf
http://umpir.ump.edu.my/id/eprint/20675/7/Transdermal%20delivery%20of%20raloxifene%20HCl%20via%20ethosomal%20system.%20Formulation%2Cadvanced%20characterizations%20and%20pharmacokinetic%20evaluation.pdf
first_indexed 2023-09-18T22:29:57Z
last_indexed 2023-09-18T22:29:57Z
_version_ 1777416219254587392

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