Microsponges are drug delivery systems that improve drug stability and slow the release rate. Favipiravir (antiviral) microsponges are prepared by the emulsion solvent diffusion method using ethyl cellulose and PVA. Optimization was done by using the Box-Behnken design. Favipiravir microsponges were evaluated for physicochemical parameters, nebulization time (11.6–17.28 minutes), aerosol mass output (0.912%–4.337%), aerosol output rate (0.0082–-0.0187 mg/minute), and respirable fraction (0.535%–2.423%). Based on these criteria of maximum percentage yield, maximum entrapment efficiency, and minimum drug release for 8 hours, the solution with desirability of 0.900 was given. The optimized favipiravir microsponge formulation (PMS) was prepared with the composition of ethyl cellulose (372 mg), PVA (248 mg), and speed (1222 RPM) and evaluated, showed percentage yield of (87.16% ± 0.020%), entrapment efficiency (95.14% ± 0.16%), assay (94.69% ± 0.23%) in-vitro drug release within 8 hours (44.043% ± 0.18%). DSC and XRD studies confirmed the amorphous form of the drug and its compatibility with the excipients used. Thermogravimetric analysis studies showed weight loss in the region of 300°C– 400°C, which indicates degradation and differential thermal analysis effects were observed at 650°C–670°C corresponding to recrystallization of dehydrated material. Thermal analysis and stability studies indicate microsponges are stable even at higher temperatures. The Zeta potential of the optimized formulation (+1.04 mv) indicates stability. SEM of the optimized formulation showed a smooth surface and swelling of the microsponges under the twin-stage impinger stage 1 and stage 2. Favipiravir microsponges of particle size 4.394 ± 0.35 μm, with good flow properties and % EE can be targeted to the lungs.
Kothamasi P, Bandari V, Babasaheb KS, Naredla B, Shaik NB, Domaraju P. Optimization of favipiravir microsponges for pulmonary drug delivery. J Appl Pharm Sci. 2024. Online First. http://doi.org/10.7324/JAPS.2025.206181
1. Shah ND, Shah VV, Chivate ND. Pulmonary drug delivery: a promising approach. J Appl Pharm Sci. 2012;02(06):33–7. doi: https://doi.org/10.7324/JAPS.2012.2632
2. Agrawal U, Raju R, Udwadia ZF. Favipiravir: a new and emerging antiviral option in COVID-19. Med J Armed Forces India. 2020 Oct;76(4):370–6. doi: https://doi.org/10.1016/j.mjafi.2020.08.004
3. Hung DT, Ghula S, Aziz JMA, Makram AM, Tawfik GM, Abozaid AA, et al. The efficacy and adverse effects of favipiravir on patients with COVID-19: a systematic review and meta-analysis of published clinical trials and observational studies. Int J Infect Dis. 2022 Jul;120:217–27. doi: https://doi.org/10.1016/j.ijid.2022.04.035
4. Lau M, Young PM, Traini D. A review of co-milling techniques for the production of high dose dry powder inhaler formulation. Drug Dev Ind Pharm. 2017 Aug;43(8):1229–38. doi: https://doi.org/10.1080/03639045.2017.1313858
5. Bhatia M, Saini M. Formulation and evaluation of curcumin microsponges for oral and topical drug delivery. Prog Biomatter. 2018 Sep;7(3):239–48. doi: https://doi.org/10.1007/s40204-018-00999
6. Gade R, Nama S, Avula PR. Formulation development and evaluation of once daily fexofenadine hydrochloride microsponge tablets. Trends Sci. 2022;20(1):4271. doi: https://doi.org/10.48048/tis.2023.4271
7. Moin A, Roohi NKF, Rizvi SMD, Ashraf SA, Siddiqui AJ, Patel M, et al. Design and formulation of polymeric nanosponges tablets with enhanced solubility for combination therapy. RSC Adv. 2020 Sep 21;10(57):34869–84. doi: https://doi.org/10.1039/d0ra06611g
8. Como?lu T, Gönül N, Baykara T. Preparation and in-vitro evaluation of modified release ketoprofen microsponges. Farmaco. 2003 Feb;58(2):101–6. doi: https://doi.org/10.1016/s0014-827x(02)00007-1
9. Ibrahim B. HPLC-UV method for quantification of favipiravir in pharmaceutical formulations. Acta Chromatogr. 2021;33(3)209–15. doi: https://doi.org/10.1556/1326.2020.00828
10. Subrahmanyam CVS. Micromeritics. Text book of Physical Pharmaceutics, 2nd ed. Delhi, India: VallabhPrakashan publishers; 2000.
11. Mali AJ, Rokade A, Kamble R, Pawar A, Bothiraja C. Resveratrol-loaded microsponge as a novel biodegradable carrier for dry powder inhaler: a new strategy in lung delivery. Bio Nanosci. 2021;11:1–12. doi: https://doi.org/10.1007/s12668-020-00800-7
12. Khan I, Lau K, Bnyan R, Houacine C, Roberts M, Isreb A, et al. A facile and novel approach to manufacture paclitaxel-loaded proliposome tablet formulations of micro or nano vesicles for nebulization. Pharm Res. 2020 Jun 2;37(6):116. doi: https://doi.org/10.1007/s11095-020-02840-w
13. Pandey P, Mishra S, Anupriya K, Sharma N, Kumari Ppa. Tolnaftate microsponges embedded biocompatible gels for controlled and effective antidermatophytic activity. Int Res J Pharm. 2018;9(6):128–33. doi: https://doi.org/10.7897/2230-8407.096103
14. Mahant S, Kumar S, Nanda S, Rao R. Microsponges for dermatological applications: perspectives and challenges. Asian J Pharm Sci. 2020;15(3):273–91. doi: https://doi.org/10.1016/j.ajps.2019.05.004
15. Suryanarayana R. X ray powder diffractometry physical characterization of pharmaceutical solids. Boca Raton, FL: CRC press; 1995. pp 187–221.
16. Giordano F, Novak C, Moyano JR. Thermal analysis of cyclodextrins and their inclusion compounds. Thermochimica Acta. 2001;380(2):123–51. doi: https://doi.org/10.1016/S0040-6031(01)00665-7
17. Raut AV, Kathar N, Sanap G. Microsponges: the drug delivery system. Int J Pharm Sci. 2024;2(1):328–41. doi: https://doi.org/10.5281/zenodo.10523750
18. Vidya KP, Gopinath E, Nesalin JA, Chandy V. Unveiling the potential of microsponges: enhancing oral bioavailability. World J Biol Pharm Health Sci. 2024;17(02):405–14. doi: https://doi.org/10.30574/wjbphs.2024.17.2.0085
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