Formulation and Evaluation of Self-Nanoemulsifying Drug Delivery System Derived Tablet Containing Sertraline

Anroop B Nair; Bhavna Singh; Jigar Shah; Shery Jacob; Bandar Aldhubiab; Nagaraja Sreeharsha; Mohamed A Morsy; Katharigatta N Venugopala; Mahesh Attimarad; Pottathil Shinu

doi:10.3390/pharmaceutics14020336

Formulation and Evaluation of Self-Nanoemulsifying Drug Delivery System Derived Tablet Containing Sertraline

Pharmaceutics. 2022 Jan 31;14(2):336. doi: 10.3390/pharmaceutics14020336.

Authors

Affiliations

¹ Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
² Department of Pharmaceutics, Institute of Pharmacy, Nirma University, Ahmedabad 382481, India.
³ Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman P.O. Box 4184, United Arab Emirates.
⁴ Department of Pharmaceutics, Vidya Siri College of Pharmacy, Off Sarjapura Road, Bangalore 560035, India.
⁵ Department of Pharmacology, Faculty of Medicine, Minia University, El-Minia 61511, Egypt.
⁶ Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4000, South Africa.
⁷ Department of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.

Abstract

Being a biopharmaceutics classification system class II drug, the absorption of sertraline from the gut is mainly limited by its poor aqueous solubility. The objective of this investigation was to improve the solubility of sertraline utilizing self-nanoemulsifying drug delivery systems (SNEDDS) and developing it into a tablet dosage form. Ternary phase diagrams were created to identify nanoemulsion regions by fixing oil (glycerol triacetate) and water while varying the surfactant (Tween 80) and co-surfactant (PEG 200) ratio (S_mix). A three-factor, two-level (2³) full factorial design (batches F1-F8) was utilized to check the effect of independent variables on dependent variables. Selected SNEDDS (batch F4) was solidified into powder by solid carrier adsorption method and compressed into tablets. The SNEDDS-loaded tablets were characterized for various pharmaceutical properties, drug release and evaluated in vivo in Wistar rats. A larger isotropic region was noticed with a S_mix ratio of 2:1 and the nanoemulsion exhibited good stability. Screening studies' data established that all three independent factors influence the dependent variables. The prepared tablets displayed optimal pharmaceutical properties within acceptable limits. In vitro sertraline release demonstrated from solid SNEDDS was statistically significant (p < 0.0001) as compared to pure sertraline. Differential Scanning Calorimetry and X-Ray Diffraction data established the amorphous state of the drug in SNEDDS formulation, while FTIR spectra indicate the compatibility of excipients and drug. Pharmacokinetic evaluation of the SNEDDS tablet demonstrated significant increment (p < 0.0001) in AUC_0-_α (~5-folds), C_max (~4-folds), and relative bioavailability (386%) as compared to sertraline suspension. The current study concludes that the solid SNEDDS formulation could be a practicable and effective strategy for oral therapy of sertraline.

Keywords: bioavailability; full factorial design; nanoemulsion; pharmacokinetics; self-nanoemulsifying tablets; sertraline.

Grants and funding

1811021/Deanship of Scientific Research, King Faisal University