Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)

Orthosiphon stamineus Benth (O.S) is a traditional south-east Asian herb. The extract of O.S is used in the formulation of ethanolic nanolipid vesicle system to have considerable potential for tumour therapeutics. Methods: The research objective is to develop and characterise the anticancer and anti...

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Main Authors: Nazari, V. Mansoureh, Mahmood, Syed, Shah, Amin Malik, Al-Suede, Fouad Saleh Resq
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Published: Bentham Science Publ Ltd 2022
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Online Access:http://eprints.um.edu.my/41471/
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spelling my.um.eprints.414712023-09-25T03:09:10Z http://eprints.um.edu.my/41471/ Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome) Nazari, V. Mansoureh Mahmood, Syed Shah, Amin Malik Al-Suede, Fouad Saleh Resq QD Chemistry R Medicine RM Therapeutics. Pharmacology Orthosiphon stamineus Benth (O.S) is a traditional south-east Asian herb. The extract of O.S is used in the formulation of ethanolic nanolipid vesicle system to have considerable potential for tumour therapeutics. Methods: The research objective is to develop and characterise the anticancer and antiangiogenic effect of O.S extract in the form of nano-ethanolic spherosomes (ESP) using phospholipids in melanoma. Spherosomes formulation of O.S was developed using the thin-film re-hydration method and converted to gel using Acrypol 1%. The formulations were subjected to optimisation and physical-chemical characterisations like particle size, surface charge, DSC, FTIR, and TEM. Cytotoxicity of O.S and ESP was studied using an endothelial cell line (EA. hy926). Furthermore, anti-melanoma effect of O.S spherosome gel was studied in albino mice after topical administration. Results: ESP-6 with the ratio of extract (O.S): cholesterol: phospholipid (1: 6: 0.5) showed the highest entrapment efficiency (80.56 +/- 0.84%) using ultraviolet spectroscopy. In-vivo permeation/penetration studies revealed deeper absorption of ESP-6 compared to a hydroethanolic gel of O.S. In-vitro and in vivo anti-melanoma studies demonstrated the significant tumour-suppressing effect of ESP-6 on murine melanoma. Percentage inhibition of tumour growth by O.S and ESP-6 at 3000 mg/kg showed to be 63.98 +/- 7.86% and 87.76 +/- 7.90%, respectively. Conclusion: Spherosome vesicles were developed with a smooth surface. The results demonstrated that O.S extract showed no toxicity when tested on the endothelial cell line. O.S loaded in spherosomes has the potential to lower the growth of melanoma in mice. The spherosomes loaded with O.S do not promote tumour growth or act as antiangio-genetic in melanoma. Bentham Science Publ Ltd 2022-04 Article PeerReviewed Nazari, V. Mansoureh and Mahmood, Syed and Shah, Amin Malik and Al-Suede, Fouad Saleh Resq (2022) Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome). Current Drug Metabolism, 23 (4). pp. 317-328. ISSN 1389-2002, DOI https://doi.org/10.2174/1389200223666220416215129 <https://doi.org/10.2174/1389200223666220416215129>. 10.2174/1389200223666220416215129
institution Universiti Malaya
building UM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Malaya
content_source UM Research Repository
url_provider http://eprints.um.edu.my/
topic QD Chemistry
R Medicine
RM Therapeutics. Pharmacology
spellingShingle QD Chemistry
R Medicine
RM Therapeutics. Pharmacology
Nazari, V. Mansoureh
Mahmood, Syed
Shah, Amin Malik
Al-Suede, Fouad Saleh Resq
Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)
description Orthosiphon stamineus Benth (O.S) is a traditional south-east Asian herb. The extract of O.S is used in the formulation of ethanolic nanolipid vesicle system to have considerable potential for tumour therapeutics. Methods: The research objective is to develop and characterise the anticancer and antiangiogenic effect of O.S extract in the form of nano-ethanolic spherosomes (ESP) using phospholipids in melanoma. Spherosomes formulation of O.S was developed using the thin-film re-hydration method and converted to gel using Acrypol 1%. The formulations were subjected to optimisation and physical-chemical characterisations like particle size, surface charge, DSC, FTIR, and TEM. Cytotoxicity of O.S and ESP was studied using an endothelial cell line (EA. hy926). Furthermore, anti-melanoma effect of O.S spherosome gel was studied in albino mice after topical administration. Results: ESP-6 with the ratio of extract (O.S): cholesterol: phospholipid (1: 6: 0.5) showed the highest entrapment efficiency (80.56 +/- 0.84%) using ultraviolet spectroscopy. In-vivo permeation/penetration studies revealed deeper absorption of ESP-6 compared to a hydroethanolic gel of O.S. In-vitro and in vivo anti-melanoma studies demonstrated the significant tumour-suppressing effect of ESP-6 on murine melanoma. Percentage inhibition of tumour growth by O.S and ESP-6 at 3000 mg/kg showed to be 63.98 +/- 7.86% and 87.76 +/- 7.90%, respectively. Conclusion: Spherosome vesicles were developed with a smooth surface. The results demonstrated that O.S extract showed no toxicity when tested on the endothelial cell line. O.S loaded in spherosomes has the potential to lower the growth of melanoma in mice. The spherosomes loaded with O.S do not promote tumour growth or act as antiangio-genetic in melanoma.
format Article
author Nazari, V. Mansoureh
Mahmood, Syed
Shah, Amin Malik
Al-Suede, Fouad Saleh Resq
author_facet Nazari, V. Mansoureh
Mahmood, Syed
Shah, Amin Malik
Al-Suede, Fouad Saleh Resq
author_sort Nazari, V. Mansoureh
title Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)
title_short Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)
title_full Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)
title_fullStr Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)
title_full_unstemmed Suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)
title_sort suppression of melanoma growth in a murine tumour model using orthosiphon stamineus benth. extract loaded in ethanolic phospholipid vesicles (spherosome)
publisher Bentham Science Publ Ltd
publishDate 2022
url http://eprints.um.edu.my/41471/
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score 13.211869