EVALUATION OF MICROSPHERE OF POLY(LACTIC ACID) AS CELECOXIB CARRIER

Authors

  • lany nurhayati Department of Chemistry, Faculty of Mathematic of Natural Sciences, Nusa Bangsa University, Jalan KH Sholeh Iskandar Km 4, Bogor 16166, Indonesia, Indonesia
  • Suminar S. Achmadi Department of Chemistry, Faculty of Mathematic of Natural Sciences, IPB University, IPB Dramaga Campus, Jalan Tanjung, Bogor 16680, Indonesia
  • Sudaryanto Sudaryanto Research Center for Advanced Materials, National Research and Innovation Agency, Gedung Manajemen (Gedung 720), Jalan Puspiptek Raya No. 60, Banten 15314, Indonesia

DOI:

https://doi.org/10.15575/ak.v11i2.39310

Keywords:

poly(lactic acid), microspheres, celecoxib, slow release.

Abstract

Celecoxib, cyclooxygenase-2 inhibitor approved for the management of rheumatism and osteoarthritis. Celecoxib is a Biopharmaceutics Classification System (BCS) class II compound whose oral bioavailability is highly limited owing to its poor aqueous solubility. Microencapsulation is very helpful to increase the solubility and slow the release of drugs. For the drugs of BCS Class-II, we use this technique which enables us to get more solubility and increase dissolution profile. The present study aims to reduce the drug’s negative effect and boost its bioavailability. Poly(lactic acid) (PLA) a biodegradable polymer microsphere that can be synthesized to encapsulate celecoxib, was prepared by solvent evaporation with chloroform were used. The characterized surface morphology, drug entrapment efficiency (DDE), and in vitro drug release. Morphology was studied by scanning electron microscopy (SEM), crystallinity was studied using an X-ray diffractometer (XRD), and drug release was spectrophotometer UV-Vis. The results were observed to indicate there were microspheres homogeneous in the distribution of celecoxib in the polymer matrix. Formulations indicated that DEE was between 55.80 and 70.70% with prolonged length microspheres in the 10-30 µm range. Study in vitro drug release, when placed in phosphate buffer (pH 7.4) containing 2% w/w Tween 80 solvent, there was an initial burst of drug release within the first two hours followed by constant drug release. The PLA microsphere can release the confined celecoxib gradually but does not follow a controlled diffusion mechanism, but rather a mechanism of expansion and erosion of the microsphere matrix.

Author Biography

lany nurhayati, Department of Chemistry, Faculty of Mathematic of Natural Sciences, Nusa Bangsa University, Jalan KH Sholeh Iskandar Km 4, Bogor 16166, Indonesia

Fakultas MIPA-UNB

References

A. Malik, N. Parvez, and P. Kumar Sharma, “Novel Methods of Microsphere Formulation,†World Appl. Sci. J., 32(5), pp. 839–847, 2014, doi: 10.5829/idosi.wasj.2014.32.05.84139.

M. Lengyel, N. Kállai-Szabó, V. Antal, A. J. Laki, and I. Antal, “Microparticles, microspheres, and microcapsules for advanced drug delivery,†Sci. Pharm., 87(3), 2019, https://doi.org/10.3390/scipharm87030020

Y. K. Sung and S. W. Kim, “Recent advances in polymeric drug delivery systems,†Biomater. Res., 24(12), 2020, [Online]. Available: https://biomaterialsres.biomedcentral.com/articles/10.1186/s40824-020-00190-7 https://doi.org/10.1186/s40824-020-00190-7 .

P. Sharma, P. Negi, and N. Mahindroo, “Recent advances in polymeric drug delivery carrier systems,†Adv. Polym. Biomed. Appl., pp. 369–388, 2018.

G. Chandra and A. Pandey, “Biodegradable bone implants in orthopedic applications: a review,†Biocybern. Biomed. Eng., vol. 40, no. 2, pp. 596–610, 2020, https://doi.org/10.1016/j.bbe.2020.02.003 .

K. Chauhan;, J. S. Jandu;, L. H. Brent;, and M. A. Al-Dhahir., Rheumatoid arthtritis. [Online]. Available: https://www.ncbi.nlm.nih.gov/books/NBK441999/

A. P. Zahra and N. Carolia, “Obat Anti-inflamasi Non-steroid ( OAINS ): Gastroprotektif vs Kardiotoksik,†Majority, vol. 6, pp. 153–158, 2017.

M. R. Jin and Y. T. Sohn, “Crystal form of celecoxib: Preparation, characterization and dissolution,†J. Korean Chem. Soc., 62(5), pp. 352–357, 2018, https://doi.org/10.5012/jkcs.2018.62.5.352

Nidhi, M. Rashid, V. Kaur, S. S. Hallan, S. Sharma, and N. Mishra, “Microparticles as controlled drug delivery carrier for the treatment of ulcerative colitis: A brief review,†Saudi Pharm. J., 24(4), pp. 458–472, 2016, https://doi.org/10.1016/j.jsps.2014.10.001

C. Mutagond, S. Kolageri, and S. B. Katagaon, “Formulation and Evaluation of Microspheres of Ramipril,†J. Drug Deliv. Ther., 12(4)-S, pp. 23–32, 2022, https://doi.org/10.22270/jddt.v12i4-s.5486

D. M. Hariyadi et al., “Formulation, physicochemical characterisation, and in vitro evaluation of quercetin-alginate microsphere system,†Pharm. Educ., 24(3), pp. 19–24, 2024, https://doi.org/10.46542/pe.2024.243.1924

A. Rahayu, Sukarjati, P. Slamet, and N. Ambarwati, Sistem Penghantaran Obat. 2022. [Online]. Available: http://www.jstor.org/stable/resrep19672

S. Lakshmana Prabu, A. A. Shirwaikar, A. Shirwaikar, and A. Kumar, “Formulation and evaluation of sustained release microspheres of rosin containing aceclofenac,†Ars Pharm., 50(2), pp. 1–12, 2009.

P. Chaturvedi and P. Sharma, “A Review on Microencapsulation as Method of Drug Delivery,†BIO Web Conf., 86, pp. 1–15, 2024, https://doi.org/10.1051/bioconf/20248601033

A. Vlachopoulos et al., “Poly(Lactic Acid)-Based Microparticles for Drug Delivery Applications: An Overview of Recent Advances,†Pharmaceutics, 14(2), pp. 1–37, 2022, https://doi.org/10.3390/pharmaceutics14020359

R. Rabima and M. P. Sari, “Entrapment efficiency and drug loading of curcumin nanostructured lipid carrier (NLC) formula,†Pharmaciana, 9(2), p. 299, 2019, https://doi.org/10.12928/pharmaciana.v9i2.13070

H. L. Zeng, Q. Qiu, T. X. Fu, A. P. Deng, and X. Y. Xie, “Development and optimization of sustained release triptolide microspheres,†PLoS One, 18(10) October, pp. 1–20, 2023, https://doi.org/10.1371/journal.pone.0292861

N. C. Parera, “Modelling Drug Delivery Mechanisms for Microencapsulated,†TDX (Tesis Dr. en Xarxa) UPC, no. May, 2012.

M. P. Paarakh, P. A. N. I. Jose, C. M. Setty, and G. V Peter, “Release Kinetics – Concepts and Applications,†Int. J. Pharm. Res. Technol., 8(1), 2019, https://doi.org/10.31838/ijprt/08.01.02

K. M. El-Say, “Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper–Lin small composite design,†Drug Des. Devel. Ther., 10, pp. 825–839, 2016, https://doi.org/10.2147/dddt.s101900

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Published

2024-12-30

Issue

Vol. 11 No. 2 (2024): al Kimiya: Jurnal Ilmu Kimia dan Terapan

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