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Current Nanomedicine

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ISSN (Print): 2468-1873
ISSN (Online): 2468-1881

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Research Article

DoE Enabled Development and In-Vitro Optimization of Curcumin-tagged Cilostazol Solid Nano Dispersion

Author(s): Aruna Rawat, Vikas Jhawat* and Rohit Dutt

Volume 13, Issue 2, 2023

Published on: 15 August, 2023

Page: [113 - 131] Pages: 19

DOI: 10.2174/2468187313666230719121457

Price: $65

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Abstract

Background: Diabetes is a prevailing disease worldwide and its complications are also hazardous including nephropathy. Drug available to treat Diabetic Nephropathy (DN) faces bioavailability issues related to solubility and absorption of drugs. Cilostazol (CLT) is a BCS class II drug that is poorly water-soluble which affects its therapeutic efficacy. CLT reduces reactive oxygen species (ROS) increased in DN. Curcumin (Cur) is also hydrophobic but Cur has many therapeutic efficacies like anti-inflammatory and antioxidant properties that help for the treatment of DN.

Objective: The objective of the current study was to develop and optimize the Cilostazol Solid Dispersion Nanoparticle (SDN) to improve the bioavailability of the drug by tagging it with Cur by using PVP VA S 630 as polymer and Poloxamer 407 as surfactant.

Method: Different formulations were developed using the emulsion solvent evaporation method, PVP VA S 630 as the hydrophilic polymer, and Poloxamer 407 as a surfactant. Two-factor, threelevel Box-Behnken Design (BBD) was used for statistical analysis of the selected process variable's main effect and interactive effect on the response. Curcumin tagging was also done for the entire batches. Nanoparticles were characterized by FT-IR spectroscopy, DSC, Particle size, Zeta potential, Drug entrapment efficiency, Solubility, and % CDR studies.

Results: Among the 17 different formulations (CLT1-CLT 17), with a solubility of 39.5 μg/ml, a % CDR of 99.55, a typical particle size of 219.67 nm with a PDI of 0.258, entrapment efficiency of 73.47%, and a -10.6 mV of Zeta potential, CLT-15 was optimized. To determine CLT and curcumin, the simultaneous UV calibration method was created. Overall, the DSC study indicated the amorphous nature of the Nano Dispersion, which in turn means the successful entrapment of the CLT in the Nano Dispersion matrix. TEM images also confirmed the spherical nanoparticles. The optimized batch of drugs tagged with curcumin was compared with the plain drug Solid Dispersion Nanoparticles.

Conclusion: Together with the molecules of curcumin, the solid nano dispersion of CLT was produced, which will add to the benefits of the management of Diabetic Nephropathy. In the current study, we underline the importance of utilising both API and phytochemicals in the treatment of Diabetic Nephropathy, and we anticipate further basic research or clinical trials to support innovative treatments. It is possible to use these matrix-forming polymers for active ingredients with poor solubility, whether they are natural or synthetic. It has also been demonstrated that these carriers (PVP VA S 630 & Poloxamer) increase the dissolution rate (in-vitro).

Keywords: Solid dispersion nanoparticles, curcumin, response surface methodology, diabetic nephropathy, DoE, cilostazol.

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