Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluation
Ding Qu, Junjie He, Congyan Liu, Jing Zhou, Yan ChenKey Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Jiangsu, People’s Republic of ChinaAbstract: Ganoderma lucidum triterpene-loaded microemulsions (TMEs) using Coix lacrym...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Dove Medical Press
2013-12-01
|
| Series: | International Journal of Nanomedicine |
| Online Access: | http://www.dovepress.com/triterpene-loaded-microemulsion-using-coix-lacryma-jobi-seed-extract-a-a15340 |
| _version_ | 1818904737764868096 |
|---|---|
| author | Qu D He JJ Liu CY Zhou J Chen Y |
| author_facet | Qu D He JJ Liu CY Zhou J Chen Y |
| author_sort | Qu D |
| collection | DOAJ |
| description | Ding Qu, Junjie He, Congyan Liu, Jing Zhou, Yan ChenKey Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Jiangsu, People’s Republic of ChinaAbstract: Ganoderma lucidum triterpene-loaded microemulsions (TMEs) using Coix lacryma-jobi (adlay) seed oil as oil phase were prepared, characterized, and evaluated for enhanced antitumor activity. Ternary phase diagrams for the TMEs were constructed and the optimal preparation was developed. Transmission electron microscopy and dynamic light scattering showed that this formulation had a well defined spherical shape, a homogeneous distribution, a small size, and a narrow polydispersity index. The drug-loading rate was determined to be 9.87% by ultraviolet spectrophotometry, and acceptable stability under various stimulations in vitro was confirmed. Importantly, the TME formulation showed a significantly greater antiproliferative effect towards human lung carcinoma (A549) cells and murine lung tumor (Lewis) cells in comparison with suspension formulations containing triterpene and adlay seed oil as a positive control. The half-maximal inhibitory concentration of the TMEs was about 0.62 mg crude drug per mL, being 2.5-fold improved relative to that of the corresponding suspension formulation, but no significant cytotoxicity was observed for the bare microemulsion in A549 cells and Lewis cells. In vivo, the TME formulation showed markedly enhanced antitumor efficacy in a xenograft model of Lewis lung cancer after intragastric administration. Compared with cyclophosphamide, the TME formulation showed similar antitumor activity but less general toxicity. These results indicate the feasibility of using a microemulsion to increase the solubility of triterpene and adlay. TMEs hold promise as an efficient drug delivery system for the treatment of lung cancer.Keywords: microemulsion, Ganoderma lucidum, triterpene, adlay seed oil, lung cancer |
| first_indexed | 2024-12-19T21:12:12Z |
| format | Article |
| id | doaj.art-1687d2eeabbc4a169844b704e2ec52a9 |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-12-19T21:12:12Z |
| publishDate | 2013-12-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-1687d2eeabbc4a169844b704e2ec52a92022-12-21T20:05:27ZengDove Medical PressInternational Journal of Nanomedicine1178-20132013-12-012014Issue 110911915340Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluationQu DHe JJLiu CYZhou JChen YDing Qu, Junjie He, Congyan Liu, Jing Zhou, Yan ChenKey Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Jiangsu, People’s Republic of ChinaAbstract: Ganoderma lucidum triterpene-loaded microemulsions (TMEs) using Coix lacryma-jobi (adlay) seed oil as oil phase were prepared, characterized, and evaluated for enhanced antitumor activity. Ternary phase diagrams for the TMEs were constructed and the optimal preparation was developed. Transmission electron microscopy and dynamic light scattering showed that this formulation had a well defined spherical shape, a homogeneous distribution, a small size, and a narrow polydispersity index. The drug-loading rate was determined to be 9.87% by ultraviolet spectrophotometry, and acceptable stability under various stimulations in vitro was confirmed. Importantly, the TME formulation showed a significantly greater antiproliferative effect towards human lung carcinoma (A549) cells and murine lung tumor (Lewis) cells in comparison with suspension formulations containing triterpene and adlay seed oil as a positive control. The half-maximal inhibitory concentration of the TMEs was about 0.62 mg crude drug per mL, being 2.5-fold improved relative to that of the corresponding suspension formulation, but no significant cytotoxicity was observed for the bare microemulsion in A549 cells and Lewis cells. In vivo, the TME formulation showed markedly enhanced antitumor efficacy in a xenograft model of Lewis lung cancer after intragastric administration. Compared with cyclophosphamide, the TME formulation showed similar antitumor activity but less general toxicity. These results indicate the feasibility of using a microemulsion to increase the solubility of triterpene and adlay. TMEs hold promise as an efficient drug delivery system for the treatment of lung cancer.Keywords: microemulsion, Ganoderma lucidum, triterpene, adlay seed oil, lung cancerhttp://www.dovepress.com/triterpene-loaded-microemulsion-using-coix-lacryma-jobi-seed-extract-a-a15340 |
| spellingShingle | Qu D He JJ Liu CY Zhou J Chen Y Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluation International Journal of Nanomedicine |
| title | Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluation |
| title_full | Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluation |
| title_fullStr | Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluation |
| title_full_unstemmed | Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluation |
| title_short | Triterpene-loaded microemulsion using Coix lacryma-jobi seed extract as oil phase for enhanced antitumor efficacy: preparation and in vivo evaluation |
| title_sort | triterpene loaded microemulsion using coix lacryma jobi seed extract as oil phase for enhanced antitumor efficacy preparation and in vivo evaluation |
| url | http://www.dovepress.com/triterpene-loaded-microemulsion-using-coix-lacryma-jobi-seed-extract-a-a15340 |
| work_keys_str_mv | AT qud triterpeneloadedmicroemulsionusingcoixlacrymajobiseedextractasoilphaseforenhancedantitumorefficacypreparationandinvivoevaluation AT hejj triterpeneloadedmicroemulsionusingcoixlacrymajobiseedextractasoilphaseforenhancedantitumorefficacypreparationandinvivoevaluation AT liucy triterpeneloadedmicroemulsionusingcoixlacrymajobiseedextractasoilphaseforenhancedantitumorefficacypreparationandinvivoevaluation AT zhouj triterpeneloadedmicroemulsionusingcoixlacrymajobiseedextractasoilphaseforenhancedantitumorefficacypreparationandinvivoevaluation AT cheny triterpeneloadedmicroemulsionusingcoixlacrymajobiseedextractasoilphaseforenhancedantitumorefficacypreparationandinvivoevaluation |