Design and Characterization of Aceclofenac-Loaded Microballoons using Eudragit with Hydroxypropyl Methylcellulose

Authors

Abstract

Background: Drug delivery systems based on microballoons are one of the promising approaches for gastric retention, especially useful for drugs with site-specific absorption in the stomach. The microballoons are hollow, spherical particles under 200 micrometers, designed to float in the gastric environment. The Aceclofenac formulation of an NSAID is helpful with a half-life of 4–4.3 hours; this delivery form gives a sustained release and maintains constant plasma levels with enhanced bioavailability and decrease in dosing frequency.

Methodology: Microballoons of Aceclofenac were prepared using Eudragit RS 100 and Hydroxy Propyl Methyl Cellulose as polymers from the emulsion–solvent diffusion method. In this, the polymers impart stability along with a profile of controlled release. Here, the microballoons was evaluated for physical parameter and the release profile regarding average particle size, floatation percentage, entrapment efficiency, true tapped density, and percentage yield, and FTIR will be carried out on complexes of drug and polymer.

Results and Discussion: The prepared microballoons exhibit excellent floating properties and uniformity in size, which aided in long gastric retention. High entrapment efficiency with controlled and sustained release of the drug for an extended period was obtained. FTIR studies indicated that Aceclofenac remained stable in the polymer matrix with no considerable chemical interaction between the drug and the polymers.

Conclusion: This research shows promise in microballoons-based delivery systems that could maintain the release for a longer duration from the delivery device with respect to Aceclofenac, which enhances bioavailability and reduces dosing frequencies.

Keywords: Aceclofenac, Microballoons, NSAID, Sustain Release Medication, Eudragit RS100, HPMC

Keywords:

Aceclofenac, Microballoons, NSAID, Sustain Release Medication, Eudragit RS100, HPMC

DOI

https://doi.org/10.22270/jddt.v15i1.6971

Author Biographies

Souvik Biswas, Bharat Technology, Jadurberia, Uluberia, Howrah – 711316, India

Assistant Professor, Department of Pharmacology, Bharat Technology, Jadurberia, Uluberia, Howrah – 711316, India

Sindhuja Sengupta, NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

Padmanath Pegu, School of Pharmaceutical Sciences, Girijananda Chowdhury University, Tezpur Campus

School of Pharmaceutical Sciences, Girjananda Chowdhury University, Tezpur Campus, Tezpur, Bebezia Gaon, Assam–784501, India

Nikita Dey, NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

Amartya Sen, ADAMAS University, Adamas Knowledge City, Barasat - Barrackpore Road, Jagannathpur, Kolkata, West Bengal 700126

ADAMAS University, Adamas Knowledge City, Barasat - Barrackpore Road, Jagannathpur, Kolkata, West Bengal – 700126, India

Biplab Debnath, Bharat Technology, Jadurberia, Uluberia, Howrah-711316

Bharat Technology, Jadurberia, Uluberia, Howrah – 711316, India

Mrinmoy Nag, NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

Nurul Amin, NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

NEF College of Pharmaceutical Education & Research, Nagaon – 782001, India

Arijit Das, Bharat Technology, Jadurberia, Uluberia, Howrah-711316

Bharat Technology, Jadurberia, Uluberia, Howrah – 711316, India

Soumya Datta, Bharat Technology, Jadurberia, Uluberia, Howrah-711316

Bharat Technology, Jadurberia, Uluberia, Howrah – 711316, India

Amlan Bishal , Bharat Technology, Jadurberia, Uluberia, Howrah – 711316, India

Bharat Technology, Jadurberia, Uluberia, Howrah – 711316, India

References

1. Lucatelli, P., Rocco, B., Ciaglia, S., Damato, E., Mosconi, C., Argirò, R., & Catalano, C., Microballoon Interventions for Liver Tumors: Review of Literature and Future Perspectives, Journal of Clinical Medicine, 2022; 11(18): 5334. https://doi.org/10.3390/jcm11185334 PMid:36142980 PMCid:PMC9505296

2. Kállai-Szabó, N., Farkas, D., Lengyel, M., Basa, B., Fleck, C., & Antal, I., Microparticles and multi-unit systems for advanced drug delivery, European Journal of Pharmaceutical Sciences, 2024; 194(1 March): 106704. https://doi.org/10.1016/j.ejps.2024.106704 PMid:38228279

3. Mehrotra, S., Kalyan Bg, P., Nayak, P. G., Joseph, A., & Manikkath, J., Recent Progress in the Oral Delivery of Therapeutic Peptides and Proteins: Overview of Pharmaceutical Strategies to Overcome Absorption Hurdles, Advanced Pharmaceutical Bulletin, 2024; 14(1): 11-33. https://doi.org/10.34172/apb.2024.009 PMid:38585454 PMCid:PMC10997937

4. Dan, N., Samanta, K., & Almoazen, H., An Update on Pharmaceutical Strategies for Oral Delivery of Therapeutic Peptides and Proteins in Adults and Pediatrics, Children, 2020; 7(12): 307. https://doi.org/10.3390/children7120307 PMid:33352795 PMCid:PMC7766037

5. Ghlichloo I, Gerriets V. Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), In: StatPearls. Treasure Island (FL): StatPearls Publishing; May 1, 2023.

6. Iolascon, G., Giménez, S., & Mogyorósi, D., A Review of Aceclofenac: Analgesic and Anti-Inflammatory Effects on Musculoskeletal Disorders, Journal of Pain Research, 2021; 14: 3651-3663. https://doi.org/10.2147/JPR.S326101 PMid:34876850 PMCid:PMC8643213

7. Rahim, H., Sadiq, A., Ullah, R., Bari, A., Amin, F., Farooq, U., Jan, N. U., & Mahmood, H. M., Formulation of Aceclofenac Tablets Using Nanosuspension as Granulating Agent: An Attempt to Enhance Dissolution Rate and Oral Bioavailability, International Journal of Nanomedicine, 2020; 15: 8999-9009. https://doi.org/10.2147/IJN.S270746 PMid:33235448 PMCid:PMC7680606

8. Moin, A., Roohi, N. K. F., Rizvi, S. M. D., Ashraf, S. A., Siddiqui, A. J., Patel, M., Ahmed, S. M., Gowda, D. v., & Adnan, M., Design and formulation of polymeric nanosponge tablets with enhanced solubility for combination therapy, RSC Advances, 2020; 10(57): 34869-34884. https://doi.org/10.1039/D0RA06611G PMid:35514416 PMCid:PMC9056836

9. Ikechukwu, U. R., Emeka, D., Francis, J., & Aa, A., Development and Evaluation of Ritonavir Hollow Microballoons for Floating Drug Delivery, Universal Journal of Pharmaceutical Research, 2017; 2(2): 30-34. https://doi.org/10.22270/ujpr.v2i2.R3

10. Vidyadhara, S., Sasidhar, R. L., Balakrishna, T., Balaji, B., & Amrutha, R., Formulation and Evaluation of Controlled Release Floating Microballoons of Stavudine, Scientia Pharmaceutica, 2015; 83(4): 671-682. https://doi.org/10.3797/scipharm.1501-07 PMid:26839847 PMCid:PMC4727757

11. Bhuvaneswari, S., Manivannan, S., Akshay, M., & Nify, F., Formulation and Evaluation of Gastroretentive Microballoons of Acebrophylline for The Treatment of Bronchial Asthma, Asian Journal of Pharmaceutical and Clinical Research, 2016; 9(5): 105-111. https://doi.org/10.22159/ajpcr.2016.v9i5.12603

12. Usha, A. L., Karumoju, N., Rani, E. R., Andra, P. A. S. E., Review on non-effervescent gastro retentive drug delivery systems-microballons, Asian Journal of Pharmaceutical Research, 2020; 10(4): 312-318. https://doi.org/10.5958/2231-5691.2020.00053.2

13. Sato, Y., Kawashima, Y., Takeuchi, H., & Yamamoto, H., In vitro evaluation of floating and drug releasing behaviors of hollow microspheres (microballoons) prepared by the emulsion solvent diffusion method, European Journal of Pharmaceutics and Biopharmaceutics, 2004; 57(2): 235-243. https://doi.org/10.1016/S0939-6411(03)00185-1 PMid:15018980

14. Kumar, R., Kamboj, S., Chandra, A., Gautam, P. K., & Sharma, V. K., Microballoons: An Advance Avenue for Gastroretentive Drug Delivery System- A Review, Pharmaceutical and Biosciences Journal, 2016; 4(4): 29-40. https://doi.org/10.20510/ukjpb/4/i4/110644

15. Porwal, A., Swami, G., Saraf, S., Preparation and evaluation of sustained release microballoons of propranolol, Daru, 2011; 19(3):193-201. https://pubmed.ncbi.nlm.nih.gov/22615657/

16. Patel, S., Aundhia, C., Seth, D., Shah, N., Pandya, K., Shah, C., Ramani, V., Javia, A., Microballoons: A Novel Approach in Gastro-Retention Floatingdrug Delivery System (FDDS), An International Journal of Pharmaceutical Sciences, 2016; 7(2): 332-345.

Published

15-01-2025
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How to Cite

1.
Biswas S, Sengupta S, Pegu P, Dey N, Sen A, Debnath B, et al. Design and Characterization of Aceclofenac-Loaded Microballoons using Eudragit with Hydroxypropyl Methylcellulose. J. Drug Delivery Ther. [Internet]. 2025 Jan. 15 [cited 2025 Feb. 7];15(1):130-41. Available from: https://jddtonline.info/index.php/jddt/article/view/6971

How to Cite

1.
Biswas S, Sengupta S, Pegu P, Dey N, Sen A, Debnath B, et al. Design and Characterization of Aceclofenac-Loaded Microballoons using Eudragit with Hydroxypropyl Methylcellulose. J. Drug Delivery Ther. [Internet]. 2025 Jan. 15 [cited 2025 Feb. 7];15(1):130-41. Available from: https://jddtonline.info/index.php/jddt/article/view/6971

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