Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations

The study aimed to prepare and optimize luteolin (LUT)-loaded transdermal elastic liposomes (LEL1-LEL12), followed by in vitro and ex vivo evaluations of their ability to control breast cancer. Various surfactants (Span 60, Span 80, and Brij 35), and phosphatidyl choline (PC) as a lipid, were used t...

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Autores principales:	Mohammad A. Altamimi, Afzal Hussain, Mohammad AlRajhi, Sultan Alshehri, Syed Sarim Imam, Wajhul Qamar
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	luteolin elastic liposomes design expert-based optimization ex vivo permeation and drug deposition cytotoxicity against MCF-7 Medicine R Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/abb5ea548beb46fab63f69eefc9fd479
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spelling	oai:doaj.org-article:abb5ea548beb46fab63f69eefc9fd4792021-11-25T18:39:40ZLuteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations10.3390/ph141111431424-8247https://doaj.org/article/abb5ea548beb46fab63f69eefc9fd4792021-11-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1143https://doaj.org/toc/1424-8247The study aimed to prepare and optimize luteolin (LUT)-loaded transdermal elastic liposomes (LEL1-LEL12), followed by in vitro and ex vivo evaluations of their ability to control breast cancer. Various surfactants (Span 60, Span 80, and Brij 35), and phosphatidyl choline (PC) as a lipid, were used to tailor various formulation as dictated by “Design Expert<sup>®</sup> software (DOE). These were characterized for size, polydispersity index (PDI), and zeta potential. The optimized formulation (OLEL1) was selected for comparative investigations (in vitro and ex vivo) against lipo (conventional liposomes) and drug suspension (DS). Moreover, the in vitro anticancer activity of OLEL1 was compared against a control using MCF-7 cell lines. Preliminary selection of the suitable PC: surfactant ratio for formulations F1–F9 showed relative advantages of Span 80. DOE suggested two block factorial designs with four center points to identify the design space and significant factors. OLEL1 was the most robust with high functional desirability (0.95), minimum size (202 nm), relatively high drug release, increased drug entrapment (92%), and improved permeation rate (~3270 µg/cm<sup>2</sup>) as compared with liposomes (~1536 µg/cm<sup>2</sup>) over 24 h. OLEL1 exhibited a 6.2- to 2.9-fold increase in permeation rate as compared with DS (drug solution). The permeation flux values of OLEL1, and lipo were found to be 136.3, 64 and 24.3 µg/h/cm<sup>2</sup>, respectively. The drug disposition values were 670 µg, 473 µg and 148 µg, for OLEL1, lipo and DS, respectively. Thus, ex vivo parameters were significantly better for OLEL1 compared with lipo and DS which is attributed to the flexibility and deformability of the optimized formulation. Furthermore, OLEL1 was evaluated for anticancer activity and showed maximized inhibition as compared with DS. Thus, elastic liposomes may be a promising approach for improved transdermal delivery of luteolin, as well as enhancing its therapeutic efficacy in controlling breast cancer.Mohammad A. AltamimiAfzal HussainMohammad AlRajhiSultan AlshehriSyed Sarim ImamWajhul QamarMDPI AGarticleluteolinelastic liposomesdesign expert-based optimizationex vivo permeation and drug depositioncytotoxicity against MCF-7MedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1143, p 1143 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	luteolin elastic liposomes design expert-based optimization ex vivo permeation and drug deposition cytotoxicity against MCF-7 Medicine R Pharmacy and materia medica RS1-441
spellingShingle	luteolin elastic liposomes design expert-based optimization ex vivo permeation and drug deposition cytotoxicity against MCF-7 Medicine R Pharmacy and materia medica RS1-441 Mohammad A. Altamimi Afzal Hussain Mohammad AlRajhi Sultan Alshehri Syed Sarim Imam Wajhul Qamar Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations
description	The study aimed to prepare and optimize luteolin (LUT)-loaded transdermal elastic liposomes (LEL1-LEL12), followed by in vitro and ex vivo evaluations of their ability to control breast cancer. Various surfactants (Span 60, Span 80, and Brij 35), and phosphatidyl choline (PC) as a lipid, were used to tailor various formulation as dictated by “Design Expert<sup>®</sup> software (DOE). These were characterized for size, polydispersity index (PDI), and zeta potential. The optimized formulation (OLEL1) was selected for comparative investigations (in vitro and ex vivo) against lipo (conventional liposomes) and drug suspension (DS). Moreover, the in vitro anticancer activity of OLEL1 was compared against a control using MCF-7 cell lines. Preliminary selection of the suitable PC: surfactant ratio for formulations F1–F9 showed relative advantages of Span 80. DOE suggested two block factorial designs with four center points to identify the design space and significant factors. OLEL1 was the most robust with high functional desirability (0.95), minimum size (202 nm), relatively high drug release, increased drug entrapment (92%), and improved permeation rate (~3270 µg/cm<sup>2</sup>) as compared with liposomes (~1536 µg/cm<sup>2</sup>) over 24 h. OLEL1 exhibited a 6.2- to 2.9-fold increase in permeation rate as compared with DS (drug solution). The permeation flux values of OLEL1, and lipo were found to be 136.3, 64 and 24.3 µg/h/cm<sup>2</sup>, respectively. The drug disposition values were 670 µg, 473 µg and 148 µg, for OLEL1, lipo and DS, respectively. Thus, ex vivo parameters were significantly better for OLEL1 compared with lipo and DS which is attributed to the flexibility and deformability of the optimized formulation. Furthermore, OLEL1 was evaluated for anticancer activity and showed maximized inhibition as compared with DS. Thus, elastic liposomes may be a promising approach for improved transdermal delivery of luteolin, as well as enhancing its therapeutic efficacy in controlling breast cancer.
format	article
author	Mohammad A. Altamimi Afzal Hussain Mohammad AlRajhi Sultan Alshehri Syed Sarim Imam Wajhul Qamar
author_facet	Mohammad A. Altamimi Afzal Hussain Mohammad AlRajhi Sultan Alshehri Syed Sarim Imam Wajhul Qamar
author_sort	Mohammad A. Altamimi
title	Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations
title_short	Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations
title_full	Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations
title_fullStr	Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations
title_full_unstemmed	Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations
title_sort	luteolin-loaded elastic liposomes for transdermal delivery to control breast cancer: in vitro and ex vivo evaluations
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/abb5ea548beb46fab63f69eefc9fd479
work_keys_str_mv	AT mohammadaaltamimi luteolinloadedelasticliposomesfortransdermaldeliverytocontrolbreastcancerinvitroandexvivoevaluations AT afzalhussain luteolinloadedelasticliposomesfortransdermaldeliverytocontrolbreastcancerinvitroandexvivoevaluations AT mohammadalrajhi luteolinloadedelasticliposomesfortransdermaldeliverytocontrolbreastcancerinvitroandexvivoevaluations AT sultanalshehri luteolinloadedelasticliposomesfortransdermaldeliverytocontrolbreastcancerinvitroandexvivoevaluations AT syedsarimimam luteolinloadedelasticliposomesfortransdermaldeliverytocontrolbreastcancerinvitroandexvivoevaluations AT wajhulqamar luteolinloadedelasticliposomesfortransdermaldeliverytocontrolbreastcancerinvitroandexvivoevaluations
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Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations

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