Adv Pharm Bull. 2020;10(3): 408-417.
doi: 10.34172/apb.2020.049
PMID: 32665899
PMCID: PMC7335978
Scopus ID: 85088615949
  Abstract View: 985
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Research Article

Formulation and In Vitro Evaluation of Casein Nanoparticles as Carrier for Celecoxib

Jyotsana R. Madan 1* ORCID logo, Izharahemad N. Ansari 1, Kamal Dua 2 ORCID logo, Rajendra Awasthi 3 ORCID logo

1 Department of Pharmaceutics, Smt. Kashibai Navale College of Pharmacy, Savitribai Phule Pune University, Pune 411048, Maharashtra, India.
2 Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo NSW 2007, Australia.
3 Amity Institute of Pharmacy, Amity University Uttar Pradesh, Noida 201313, India.
*Corresponding Author: *Corresponding Author: Jyotsana R. Madan, Tel.: +91-9420148817, Email:, Email: jyotsna.madan@sinhgad.edu


Purpose: The objective of this work was to formulate casein (CAS) nanocarriers for the dissolution enhancement of poorly water soluble drug celecoxib (CLXB).

Methods: The CLXB loaded CAS nanocarriers viz., nanoparticles, reassembled CAS micelles and nanocapsules were prepared using sodium caseinate (SOD-CAS) as a carrier to enhance the solubility of CLXB. The prepared formulations were characterized for particle size, polydispersity index, zeta potential, percentage entrapment efficiency, and surface morphology for the selection of best formulation. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction study was used to for the confirmation of encapsulation of CLXB. Further, in vitro drug dissolution, ex-vivo permeation studies on chicken ileum and stability studies were carried out.

Results: The CLXB loaded casein nanoparticles (CNP) (batch A2) showed a particle size diameter 216.1 nm, polydispersity index 0.422 with percentage entrapment efficiency of 90.71% and zeta potential of -24.6 mV. Scanning electron microscopy of suspension confirmed globular shape of CNP. The in vitro release data of optimized batch followed non Fickian diffusion mechanism. The ex vivo permeation studies on chicken ileum of CLXB loaded CNP showed permeation through mucous membrane as compared to pure CLXB. The apparent permeability of best selected freeze dried CLXB loaded CNP (batch A2) was higher and gradually increased from 0.90 mg/cm2 after 10 min to a maximum of 1.95 mg/cm2 over the subsequent 90 min. A higher permeation was recorded at each time point than that of the pure CLXB.

Conclusion: The study explored the potential of CAS as a carrier for solubility enhancement of poorly water soluble drugs.

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Submitted: 28 Jul 2019
Revision: 28 Jan 2020
Accepted: 03 Feb 2020
ePublished: 11 May 2020
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