title: Pharmacokinetics study of arteether loaded solid lipid nanoparticles: an improved oral bioavailability in rats.
abstract: Arteether (ART), an artemisinin derivative, is a life saving drug for multiple drug resistant malaria. It has a deliverance effect in Falciparum malaria and cerebral malaria. We have prepared solid lipid nanoparticles (SLN) by high pressure homogenization (HPH) technique. ART-loaded SLN (ART-SLN) has been produced reproducibly with homogeneous particle size. ART-SLN was characterized for their size measured by Zetasizer Nano-ZS, Malvern, UK and by high resolution transmission electron microscopy (HR-TEM) and which was found to be 100 ± 11.2 nm. The maximum percentage entrapment efficiency (%EE) determined with the high-performance liquid chromatography (HPLC) has been found to be 69 ± 4.2% in ART-SLN-3. The release pattern from ART-SLN revealed that the release of ART is slow but time-dependent manner, which is desirable as it will help to protect the acid degradation of ART in stomach. The percentage cytotoxicity of blank SLN has been found within the acceptable range. The pharmacokinetics results indicated that ART-SLN-3 absorption has been significantly enhanced in comparison to ART in aqueous suspension and ART in ground nut oil (GNO) in rats. The % relative bioavailability (RB%) of ART-SLN to the ART in GNO and ART in aqueous suspension in rats was 169.99% and 7461%, respectively which was found to be significantly high in both the cases. From the results, it can be concluded that ART-SLN offers a new approach to improve the oral bioavailability of ART.
authors.affiliation: Pharmaceutics Division, Central Drug Research Institute, Lucknow 226031, India. Electronic address: dwivedipank@gmail.com.
authors.forename: Pankaj
authors.initials: P
authors.lastname: Dwivedi
authors.affiliation: Pharmaceutics Division, Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Renuka
authors.initials: R
authors.lastname: Khatik
authors.affiliation: Pharmaceutics Division, Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Kiran
authors.initials: K
authors.lastname: Khandelwal
authors.affiliation: Pharmacokinetics and Metabolism Division, Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Isha
authors.initials: I
authors.lastname: Taneja
authors.affiliation: Pharmacokinetics and Metabolism Division, Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Kanumuri Siva Rama
authors.initials: KS
authors.lastname: Raju
authors.affiliation: Pharmacokinetics and Metabolism Division, Central Drug Research Institute, Lucknow 226031, India.
authors.lastname: Wahajuddin
authors.affiliation: Banasthali Vidyapeeth, Banasthali, Rajasthan 304022, India.
authors.forename: Sarvesh Kumar
authors.initials: SK
authors.lastname: Paliwal
authors.affiliation: Pharmaceutics Division, Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Anil Kumar
authors.initials: AK
authors.lastname: Dwivedi
authors.affiliation: Pharmaceutics Division, Central Drug Research Institute, Lucknow 226031, India.
authors.forename: Prabhat Ranjan
authors.initials: PR
authors.lastname: Mishra
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D037621:Artemisinins / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D008055:Lipids / Q000737:chemistry; D008297:Male; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D017207:Rats, Sprague-Dawley; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D008055:Lipids; D013501:Surface-Active Agents; C055141:artemotil
keywords: Arteether; High pressure homogenizer; LC-MS; Pharmacokinetics; SLN