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Arteether nanoemulsion for enhanced efficacy against Plasmodium yoelii nigeriensis malaria: An approach by enhanced bioavailability

หน่วยงาน Central Drug Research Institute (CDRI), India

รายละเอียด

ชื่อเรื่อง : Arteether nanoemulsion for enhanced efficacy against Plasmodium yoelii nigeriensis malaria: An approach by enhanced bioavailability
นักวิจัย : Dwivedi, Pankaj , Khatik, Renuka , Chaturvedi, Priyanka , Khandelwal, Kiran , Taneja, Isha , Raju, K S R , Dwivedi, Hemlata , Singh, S K , Gupta, P K , Shukla, Prashant , Tripathi, Priyanka , Singh, Sarika , Tripathi, Renu , Wahajuddin , Paliwal, S K , Dwivedi, A K , Mishra, P R
คำค้น : Arteether , Nanoemulsion , High pressure homogenizer , Pharmacokinetics , LC-MS , Antimalarial efficacy
หน่วยงาน : Central Drug Research Institute (CDRI), India
ผู้ร่วมงาน : -
ปีพิมพ์ : 2558
อ้างอิง : Colloids and Surfaces B: Biointerfaces, 2015, 126, 467–475 , http://hdl.handle.net/123456789/1440
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : CSIR-CDRI Communication No. 8890
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

The present work is focused on the preparation of nanoemulsions (NEs) loaded with arteether (ART) for its enhanced efficacy against malaria parasites. ART-NEs have been prepared using high pressure homogenization (HPH) technique with the aim of improving its solubility and thus its bioavailability. ART-NEs were optimized in terms of pressure and number of cycles. Globule size and size distributions were chosen as quality parameters. The maximum drug loading was achieved up to 93±7.4% with globule size 156±10.2nm and zeta potential of -23.3±3.4mV. The developed ART-NEs were found to be stable in terms of globule size and size distribution at different pH. The in-vitro release profile of the ART-NEs showed 62% drug release within 12 h. The percentage cell viability of blank NEs were within acceptable limits. A sensitive assay method for the determination of ART in rat plasma by liquid chromatography–mass spectrometry (LC-MS) was employed after oral administration of ART-NEs. The pharmacokinetic study showed significantly enhanced bioavailability of ART in ART-NE-V. The area under curve (AUC) of ART-NE-V was AUC0-t 1988.411±119.66h.ng/ml which was significantly higher (p <0.05) than ART in ground nut oil (GNO) AUC0-t 671.852±187.05 h.ng/ml. The Cmax of ART-NE-V (1506±161.22ng/ml) was also significantly higher (p<0.05) than ART in GNO (175.2±16.54ng/ml) and ART given intramuscularly (IM) (278.05±38.59 ng/ml). The ART-NE-V was having significantly high antimalarial efficacy and survival rate of mice giving 80% cure rate at 12.5mg/kg for 5 days in comparison to 30% cure rate of ART in GNO at the same daily dose and it was also comparable to the 100% cure rate at 12.5mg/kg for 5 days for ART given intramuscularly. In conclusion ART-NE can be a promising oral delivery system for ART.

บรรณานุกรม :
Dwivedi, Pankaj , Khatik, Renuka , Chaturvedi, Priyanka , Khandelwal, Kiran , Taneja, Isha , Raju, K S R , Dwivedi, Hemlata , Singh, S K , Gupta, P K , Shukla, Prashant , Tripathi, Priyanka , Singh, Sarika , Tripathi, Renu , Wahajuddin , Paliwal, S K , Dwivedi, A K , Mishra, P R . (2558). Arteether nanoemulsion for enhanced efficacy against Plasmodium yoelii nigeriensis malaria: An approach by enhanced bioavailability.
    : Central Drug Research Institute (CDRI), India.
Dwivedi, Pankaj , Khatik, Renuka , Chaturvedi, Priyanka , Khandelwal, Kiran , Taneja, Isha , Raju, K S R , Dwivedi, Hemlata , Singh, S K , Gupta, P K , Shukla, Prashant , Tripathi, Priyanka , Singh, Sarika , Tripathi, Renu , Wahajuddin , Paliwal, S K , Dwivedi, A K , Mishra, P R . 2558. "Arteether nanoemulsion for enhanced efficacy against Plasmodium yoelii nigeriensis malaria: An approach by enhanced bioavailability".
    : Central Drug Research Institute (CDRI), India.
Dwivedi, Pankaj , Khatik, Renuka , Chaturvedi, Priyanka , Khandelwal, Kiran , Taneja, Isha , Raju, K S R , Dwivedi, Hemlata , Singh, S K , Gupta, P K , Shukla, Prashant , Tripathi, Priyanka , Singh, Sarika , Tripathi, Renu , Wahajuddin , Paliwal, S K , Dwivedi, A K , Mishra, P R . "Arteether nanoemulsion for enhanced efficacy against Plasmodium yoelii nigeriensis malaria: An approach by enhanced bioavailability."
    : Central Drug Research Institute (CDRI), India, 2558. Print.
Dwivedi, Pankaj , Khatik, Renuka , Chaturvedi, Priyanka , Khandelwal, Kiran , Taneja, Isha , Raju, K S R , Dwivedi, Hemlata , Singh, S K , Gupta, P K , Shukla, Prashant , Tripathi, Priyanka , Singh, Sarika , Tripathi, Renu , Wahajuddin , Paliwal, S K , Dwivedi, A K , Mishra, P R . Arteether nanoemulsion for enhanced efficacy against Plasmodium yoelii nigeriensis malaria: An approach by enhanced bioavailability. : Central Drug Research Institute (CDRI), India; 2558.