Article Details

FORMULATION DEVELOPMENT OF CARVEDILOL ORAL SELF-NANOEMULSION CONCENTRATE BY FULL FACTORIAL DESIGN

Kumaravelrajan R.a *, Murugan Muthukrishnanb, Poojavarshini G.a , Suba V.c , Sathishkumar T.a , Sivakumar R.a and Farzana Affrin M. F.a

a Department of Pharmaceutics, C.L. Baid Metha College of Pharmacy, affiliated to The TN DR M.G.R. Medical University, Thoraipakkam, Chennai- 600 097, Tamil Nadu, India

b Department of Formulation Research & Devolvement, Sai Mirra Innopharm Pvt. Ltd., SIDCO Estate, Ambattur, Chennai- 600 098, Tamil Nadu, India

c Department of Pharmacology, National Institute of Siddha under Ministry of Ayush, affiliated to The TN DR M.G.R. Medical University, Chennai-600 047, Tamil Nadu, India

For Correspondence: E-mail: kumaravelrajan@clbaidmethacollege.com

 

https://doi.org/10.53879/id.62.02.15089


ABSTRACT

Poor solubility of new chemical entities often leads to low bioavailability. Addressing this, selfnanoemulsifying systems for drugs like carvedilol, a cardiovascular drug, offer promising solutions. This study used a 3² factorial design to optimize a carvedilol nanoemulsion for cardiovascular disease. CCTriglyceride, Kolliphor®, and PEG 400 were identified as optimal excipients to maximize solubility. Differential Scanning Calorimetry confirmed no drug-excipient interactions. A pseudo-ternary phase diagram guided the development of a stable system, with formulation F10 achieving 95 % drug release within 30 min and minimal precipitation (1.2 %). In vitro dissolution studies showed 70 % - 90 % release within 20 min. Zeta potential analysis confirmed stability (particle size: 38.3 nm; charge: -2.059 mV). Pharmacokinetic studies in Wistar rats showed Cmax of 602.0 ng mL-1 and Tmax of 0.8 h. One-month stability tests indicated consistent appearance and drug release, with slight precipitation. This optimized nanoemulsion enhances carvedilol's bioavailability and stability, offering significant pharmaceutical potential.

Year 2025 | Volume No. 62 | Issue No.2 | Page No. 42-48
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