Sarwar Beg1,2, Hani Choudhry3, Mazin A Zamzami3, Khalid S Alharbi4, Mahfoozur Rahman5, Bhupinder Singh1,6. 1. University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160014, India. 2. Product Development Research, Jubilant Generics Limited, Noida 201301, UP, India. 3. Department of Biochemistry, Cancer Metabolism & Epigenetic Unit, Faculty of Science, Cancer & Mutagenesis Unit, King Fahd Center for Medical Research, King Abdulaziz University, Jeddah 22252, Saudi Arabia. 4. Department of Pharmacology, College of Pharmacy, Jouf University, Sakakah 72341, Saudi Arabia. 5. Department of Pharmaceutical Sciences, SIHAS, Sam Higginbottom University of Agriculture, Technology & Sciences, Allahabad 211007, UP, India. 6. UGC - Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites Biomedical Sciences, Panjab University, Chandigarh 160014, India.
Abstract
AIM: The present work involves the development of Concavalin A-conjugated nanostructured lipidic carriers (NLCs) of olmesartan medoxomil for lectin receptor targeting. MATERIALS & METHODS: Excipient selection was performed by drug solubility in solid and liquid lipids. Factor screening was carried out by evaluating the impact of formulation and process variables on the critical quality attributes. Surface modification of NLCs was carried out using Concavalin A and extensively characterized. RESULTS & CONCLUSION: NLCs exhibited the particle size of 273.6 nm, ζ-potential of -30.2 nm, encapsulation efficiency of 73.3% and sustained drug release profile. Nearly 4.2-fold improvement in cell uptake, four- to eightfold increase in Cmax and AUC, and 37% reduction in blood pressure was observed from NLCs over the pure drug.
AIM: The present work involves the development of Concavalin A-conjugated nanostructured lipidic carriers (NLCs) of olmesartanmedoxomil for lectin receptor targeting. MATERIALS & METHODS: Excipient selection was performed by drug solubility in solid and liquid lipids. Factor screening was carried out by evaluating the impact of formulation and process variables on the critical quality attributes. Surface modification of NLCs was carried out using Concavalin A and extensively characterized. RESULTS & CONCLUSION: NLCs exhibited the particle size of 273.6 nm, ζ-potential of -30.2 nm, encapsulation efficiency of 73.3% and sustained drug release profile. Nearly 4.2-fold improvement in cell uptake, four- to eightfold increase in Cmax and AUC, and 37% reduction in blood pressure was observed from NLCs over the pure drug.
Authors: Sarwar Beg; Ankit K Malik; Mohammad Javed Ansari; Asrar A Malik; Ahmed Mahmoud Abdelhaleem Ali; Abdulrahman Theyab; Mohammad Algahtani; Waleed H Almalki; Khalid S Alharbi; Sattam K Alenezi; Md Abul Barkat; Mahfoozur Rahman; Hani Choudhry Journal: ACS Omega Date: 2022-05-10