Abstract

Background: Bioactive oils of natural origin have gained huge interests from health care professionals and patients. Objective: To design a bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS) comprising curcumin (CUR) and piperine (PP) by incorporating bioactive natural oils in the formulation. Methods: The self-emulsifying properties of apricot, avocado, black seed and Zanthoxylum rhetsa seed oils were screened within various SNEDDS formulations. Each liquid SNEDDS formulation was loaded with both CUR and PP. The optimal liquid SNEDDS were solidified using Aeroperl® and Neusilin® at 1:1 w/w ratio. Liquid and solid SNEDDS were characterized by droplet size analysis, equilibrium solubility, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy. In-vitro dissolution studies were performed to evaluate the efficiency of CUR and PP release from solid Bio-SNEDDS. Results: The liquid SNEDDS comprised of black seed oil exhibited excellent self-emulsification performance, low droplet size along with transparent appearance. The inclusion of the cosolvent Transcutol P improved the solubilization capacity of both CUR and PP. The liquid SNEDDS were efficiently solidified using the two adsorbents and presented the drugs within amorphous state. In particular, SNEDDS comprised of black seed oil/Imwitor988/Transcutol P/Cremophor RH40 (20/20/10/50) and when solidified with Neusilin showed enhanced CUR and PP release (up to 60% and 77%, respectively). In addition, this formulation efficiently delivers the highly bioactive black seed oil to the patient. Conclusions: The optimized Bio-SNEDDS comprising black seed oil showed outstanding self-emulsification characteristics along with enhanced CUR/PP dissolution upon solidification.

Highlights

  • The demand for natural formulation active/inactive ingredients is increasing due to the increased risk of side effects posed by the synthetic compounds

  • The seeds of Nigella sativa (N. sativa) Linn., family Ranunculaceae were collected from the Southwest part of Bangladesh in the month of March

  • The combined dosage form of CUR-PP solid self-nanoemulsifying drug delivery systems (SNEDDS) formulation was successfully developed with increased drug solubilization and enhanced dissolution rate

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Summary

Introduction

The demand for natural formulation active/inactive ingredients is increasing due to the increased risk of side effects posed by the synthetic compounds. Various diseases (such as diabetes, cancer, stroke, Alzheimer’s and atherosclerosis), have been safely treated with natural entities and antioxidant-based formulations [1]. Bioactive natural oils play vital roles in the development of new drugs, Molecules 2020, 25, 1703; doi:10.3390/molecules25071703 www.mdpi.com/journal/molecules activity. Bioactive oils of natural origin have gained huge interests from health care professionals and patients. Objective: To design a bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS) comprising curcumin (CUR) and piperine (PP) by incorporating bioactive natural oils in the formulation. Methods: The self-emulsifying properties of apricot, avocado, black seed and Zanthoxylum rhetsa seed oils were screened within various SNEDDS formulations. SNEDDS formulation was loaded with both CUR and PP. In-vitro dissolution studies were performed to evaluate the efficiency of CUR and PP release from solid Bio-SNEDDS

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