Optimization of Formulation Variables Using Central Composite Design to Enhance Andrographolide Release from Andrographis paniculata Extract-Chitosan Solid Dispersion

Abstract:

Andrographolide (AGP), a major component of Andrographis paniculata (Burm.f.) Nees (AP), has several biological activities. Nevertheless, poorly water solubility and low bioavailability of AGP lead to decrease clinical benefits. Therefore, this study aims to develop of AP extract-chitosan solid dispersion using central composite design (CCD) to enhance AGP release. AP crude extract was obtained by Soxhlet extractor using 85%v/v ethanol as a solvent extraction. Then, AP extract, chitosan, and poloxamer 188 in the concentrations provided by CCD was spray dried. The in-vitro release of AP extract-chitosan spray dried powder was studied by dissolution equipped with enhancer cell in 200 ml of 50%v/v methanol at 37°C and 50 rpm of paddle speed. Samples were withdrawn at 0.25-96 hours and then determined AGP by UV spectrophotometer at 224 nm. The results of CCD indicated that %ethanol and %AGP from concentrated AP extract had significant (P < 0.05) effect on the concentration of AGP released at 5 hours. The optimum formulation composed of %ethanol of 18.25, %AGP in extract of 0.38, and %poloxamer 188 of 0.17 resulted in more AGP concentration at 5 hours than 50 μg/mL. Release kinetic study revealed that %release of the optimal formulation was best fitted to first order kinetic. In powder X-ray diffraction, intensity of AGP characteristic peaks in the optimal formulation decreased by 7.17-25.69 times compared with AGP standard. It was concluded that the optimal formulation of AP extract-chitosan solid dispersion could improve AGP release due to changing crystalline AGP to amorphous state.

• Periodical: Advances in Science and Technology (Volume 121)
• Pages: 9-16
• DOI: https://doi.org/10.4028/p-3xj8r7
• Online since: October 2022
• Authors: Chanicha Nontasirichayakul, Chutima Wiranidchapong*, Worapan Sithithaworn, Duangratana Shuwisitkul
• Keywords: Andrographis paniculata, Central Composite Design, Release Kinetic, Solid Dispersion

References

[1] R. Subramanian, M. Z. Asmawi, A. Sadikun, A bitter plant with a sweet future? A comprehensive review of an oriental medicinal plant: Andrographis paniculata, Phytochem. Rev. 11(2011) 39-75.

DOI: 10.1007/s11101-011-9219-z

[2] CC. Yen, YK. Liang, CP. Cheng, MC. Hsu, YT.Wu, Oral Bioavailability Enhancement and Anti-Fatigue Assessment of the Andrographolide Loaded Solid Dispersion, Int J Mol Sci. 21(2020) 1-18.

DOI: 10.3390/ijms21072506

[3] R. Sari, D. Setyawan, D. Retnowati, R. Pratiwi, Development of Andrographolide‑chitosan Solid Dispersion System: Physical Characterization, Solubility, and Dissolution Testing, Asian J. Pharm. 13(2019) 5-9.

[4] R. Sari, M.L.L. Sugiarto, W. Amirah, H. Yusuf, The effect of chitosan type and concentration on physical characteristics and drug release behavior of andrographolide-chitosan microparticles prepared by ionic gelation – freeze drying, Proceedings of ICoAPS. (2018) 60-68.

DOI: 10.2139/ssrn.3461443

[5] M. He, Z. Qin, X. Liang, X. He, B. Zhu, Z. Lu, et al, A pH-responsive mesoporous silica nanoparticles-based drug delivery system with controlled release of andrographolide for OA treatment, Regen. Biomater. 8(2021) 1-10.

DOI: 10.1093/rb/rbab020

[6] R. Sari, A. Widyawaruyanti, F.B.T. Anindita, S.K. Astuti, D. Setyawan, Development of Andrographolide-Carboxymethyl Chitosan Nanoparticles: Characterization, in vitro Release and in vivo Antimalarial Activity Study, Turk J Pharm Sci. 15(2018) 136-141.

DOI: 10.4274/tjps.53825

[7] P. Tran, Y.C. Pyo, D.H. Kim, S.E. Lee, J.K. Kim, J.S. Park, Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs, Pharmaceutics. 11(2019) 1-26.

DOI: 10.3390/pharmaceutics11030132

[8] S. Alshehri, S.S. Imam, A. Hussain, M.A. Altamimi, N.K. Alruwaili, F. Alotaibi, et al, Potential of solid dispersions to enhance solubility, bioavailability, and therapeutic efficacy of poorly water-soluble drugs: newer formulation techniques, current marketed scenario and patents, Drug Deliv. 27(2020) 1625-1643.

DOI: 10.1080/10717544.2020.1846638

[9] Y. Ma, Y. Yang, J. Xie, J. Xu, P. Yue, M. Yang, Novel nanocrystal-based solid dispersion with high drug loading, enhanced dissolution, and bioavailability of andrographolide, Int J Nanomedicine. 13(2018) 3763-3779.

DOI: 10.2147/ijn.s164228

[10] K.S. Sharma, J. Sahoo, S. Agrawal, A. Kumari, Solid dispersions: A technology for improving bioavailability, J. anal. pharm. res. 8(2019) 127-133.

DOI: 10.15406/japlr.2019.08.00326

[11] S.V. Bhujbal, B. Mitra, U. Jain, Y. Gong, A. Agrawal, S. Karki, et al, Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies, Acta Pharm Sin B. 11(2021) 2505-2536.

DOI: 10.1016/j.apsb.2021.05.014

[12] A. Kauppinen, J. Broekhuis, N. Grasmeijer, W. Tonnis, J. Ketolainen, H.W. Frijlink, et al, Efficient production of solid dispersions by spray drying solutions of high solid content using a 3-fluid nozzle, Eur J Pharm Biopharm. 123(2018) 50-58.

DOI: 10.1016/j.ejpb.2017.11.009

[13] R.H. Dave, A.D. Patel, E. Donahue, H.H. Patel, To evaluate the effect of addition of an anionic surfactant on solid dispersion using model drug indomethacin, Drug Dev Ind Pharm. 38(2012) 930-939.

DOI: 10.3109/03639045.2011.633264

[14] S.P. Chaudhari, R.P. Dugar, Application of surfactants in solid dispersion technology for improving solubility of poorly water soluble drugs, J Drug Deliv Sci Technol. 41(2017) 68-77.

DOI: 10.1016/j.jddst.2017.06.010

[15] A. Mahajan, N. Surti, P. Patel, N. Gheewala, A. Patel, D. Shah, Optimization of formulation and process variables using central composite design for the production of nevirapine spray dried solid dispersion, Dry. Technol. (2021) 1-14.

DOI: 10.1080/07373937.2021.1874408

[16] Z. Izadiyan, M. Basri, H.R. Fard Masoumi, R. Abedi Karjiban, N. Salim, K. Shameli, Modeling and optimization of nanoemulsion containing Sorafenib for cancer treatment by response surface methodology, Chem Cent J. 11(2017) 21-29.

DOI: 10.1186/s13065-017-0248-6

[17] H. Ahn, Central Composite Design for the Experiments with Replicate Runs at Factorial and Axial Points, Ind. Eng. Manag. (2015) 969-979.

DOI: 10.1007/978-3-662-47200-2_101

[18] C. Liu, K.G.H. Desai, X. Tang, X. Chen, Drug Release Kinetics of Spray-Dried Chitosan Microspheres, Dry. Technol. 24(2007) 769-776.

DOI: 10.1080/03602550600685325

[19] C. Mircioiu, V. Voicu, V. Anuta, A. Tudose, C. Celia, D. Paolino, et al, Mathematical Modeling of Release Kinetics from Supramolecular Drug Delivery Systems, Pharmaceutics. 11(2019).

DOI: 10.3390/pharmaceutics11030140

[20] M.P. Paarakh, P.A. Jose, C. Setty, G.V.P. Christoper, Release Kinetics – Concepts and Applications, Int. J. Pharm. Technol. 8(2018) 12-20.

[21] A. Okunlola, O.L. Akindele, Application of Response Surface Methodology and Central Composite Design for the Optimization of Metformin Microsphere Formulation using Tangerine (Citrus tangerina) Pectin as Copolymer, Br. J. Pharm. Res. 11(2016) 1-14.

DOI: 10.9734/bjpr/2016/25095

[22] M. Chen, C. Xie, L. Liu, Solubility of Andrographolide in Various Solvents from (288.2 to 323.2) K, J. Chem. Eng. Data. 55(2010) 5297–5298.

DOI: 10.1021/je100344z

[23] R.J. Chokshi, H. Zia, H.K. Sandhu, N.H. Shah, W.A. Malick, Improving the dissolution rate of poorly water soluble drug by solid dispersion and solid solution: pros and cons, Drug Deliv. 14(2007) 33-45.

DOI: 10.1080/10717540600640278

[24] M. Banerjee, D. Parai, S. Chattopadhyay, S.K. Mukherjee, Andrographolide: antibacterial activity against common bacteria of human health concern and possible mechanism of action, Folia Microbiol. 62(2017) 237-244.

DOI: 10.1007/s12223-017-0496-9

[25] S. Hossain, Z. Urbi, H. Karuniawati, R.B. Mohiuddin, A. Moh Qrimida, A.M.M. Allzrag, et al, Andrographis paniculata (Burm. f.) Wall. ex Nees: An Updated Review of Phytochemistry, Antimicrobial Pharmacology, and Clinical Safety and Efficacy, Life (Basel). 11(2021).

DOI: 10.3390/life11040348