ENHANCED ORAL BIOAVAILABILITY OF NANONIZED PROGESTERONE IN HEALTHY AND PREGNANT RABBITS (NPROBIO STUDY)-Reference-Cited by-同舟云学术

ENHANCED ORAL BIOAVAILABILITY OF NANONIZED PROGESTERONE IN HEALTHY AND PREGNANT RABBITS (NPROBIO STUDY)

Published:2023-01-01 Issue: Volume: Page:54-58
ISSN:
Container-title:INTERNATIONAL JOURNAL OF SCIENTIFIC RESEARCH
language:en
Short-container-title:ijsr

Author:

K Jain Gaurav¹,Sharma Jagriti¹,Modi Nimesh²,Kothari Tejas²,Hassan Nazeer³,Sharma Nitin⁴,Kesharwani Prashant³

Affiliation:

1. Center for Advanced Formulation Technology (CAFT), Delhi Pharmaceutical Science and Research University (DPSRU), Pushp Vihar, New Delhi-110017, India

2. Corona Remedies Pvt. Ltd., Mondeal Business Park, "Corona House", Block C, S. G. Highway, Apex St, near Gurudwara, Thaltej, Ahmedabad, Gujarat-380059, India

3. School of Pharmaceutical Education and Research, Jamia Hamdard, Mehrauli - Badarpur Rd, near Batra Hospital, Block D, Hamdard Nagar, New Delhi-110062, India

4. Pharmacy, Shri Ram Murti Smarak Institute of Medical Sciences, Bareilly, Uttar Pradesh 243202, Indi

Abstract

The aim of this study is to evaluate and compare the oral bioavailability of nanonized progesterone (nano-PG) and micronized progesterone (micro-PG) sustained release tablet formulation in healthy and pregnant rabbits. High pressure compressed gas technology reduces the particle size from 1.72 ± 2.5 µm (micro-PG) to 800 ± 35 nm (nano-PG). DSC and XRD showed that both micro-PG and nano-PG were crystalline and exist as form I. Higher melting enthalpy of nano-PG indicated improved drug stability whereas XRD showed slight reduction in degree of crystallinity following nanonization. Nano-PG demonstrated 2-fold higher solubility in SDS aqueous solution and signicantly higher permeability (p < 0.05) across porcine intestine compared to micro-PG. The pharmacokinetics of nano-PG and micro-PG was conducted in healthy and pregnant rabbits. The Cmax of nano-PG was higher in healthy and pregnant rabbits however the difference was signicant in healthy rabbits only. The nano-PG demonstrated 30% and 18% higher bioavailability compared to micro-PG in healthy and pregnant rabbits, respectively. In conclusion, nanonization improves solubility, dissolution and bioavailability of PG in rabbits without affecting solid state characters

Publisher

World Wide Journals

Subject

General Agricultural and Biological Sciences,Philosophy,Classics,Physical and Theoretical Chemistry,Mechanical Engineering,General Chemical Engineering,Infectious Diseases,Cell Biology,Cellular and Molecular Neuroscience,Biochemistry,Law,Social Sciences (miscellaneous),History,General Economics, Econometrics and Finance,Business and International Management,Mechanical Engineering,Ocean Engineering,Aerospace Engineering,Condensed Matter Physics,Nuclear Energy and Engineering,Civil and Structural Engineering,Statistical and Nonlinear Physics,Statistics and Probability,Industrial and Manufacturing Engineering,Management Science and Operations Research,Statistics, Probability and Uncertainty,Statistics and Probability

Reference34 articles.

1. J. K. Pru, W. Winuthayanon, J. A. M. Ii, and K. Hayashi, “Progesterone Actions and Resistance in Gynecological Disorders,” Cells 2022, Vol. 11, Page 647, vol. 11, no. 4, p. 647, Feb. 2022, doi: 10.3390/CELLS11040647.

2. X. Ruan and A. O. Mueck, “Systemic progesterone therapy—Oral, vaginal, injections and even transdermal?,” Maturitas, vol. 79, no. 3, pp. 248–255, Nov. 2014, doi: 10.1016/J.MATURITAS.2014.07.009.

3. P. D. Darney, “The androgenicity of progestins,” The American Journal of Medicine, vol. 98, no. 1, pp. S104–S110, Jan. 1995, doi: 10.1016/S0002-9343(99)80067-9.

4. V. C. Jordan, M. H. Jeng, W. H. Catherino, and C. J. Parker, “The estrogenic activity of synthetic progestins used in oral contraceptives,” Cancer, vol. 71, no. S4, pp. 1501–1505, Feb. 1993, doi: 10.1002/CNCR.2820710415.

5. M. Chambon, H. Rochefort, H. J. Vial, and D. Chalbos, “Progestins and androgens stimulate lipid accumulation in T47D breast cancer cells via their own receptors,” Journal of Steroid Biochemistry, vol. 33, no. 5, pp. 915–922, Nov. 1989, doi: 10.1016/0022-4731(89)90240-9.