Optimization and application of porous core-shell particles for direct compaction

doi:10.5246/jcps.2024.05.031

Journal of Chinese Pharmaceutical Sciences ›› 2024, Vol. 33 ›› Issue (5): 412-429.DOI: 10.5246/jcps.2024.05.031

• Original articles • Previous Articles Next Articles

Optimization and application of porous core-shell particles for direct compaction

Zhe Li¹^,^#, Yanlin Xiao¹^,^#, Lin Zhu², Wenjun Liu³, Lingyu Yang³, Zhengji Jin¹, Abid Naeem¹, Weifeng Zhu¹, Yi Feng¹^,⁴, Liangshan Ming¹^,^*()

¹ Key Laboratory of Modern Preparation of TCM, Ministry of Education, Institute for Advanced Study, Jiangxi University of Chinese Medicine, Nanchang 330004, Jiangxi, China
² Macau Centre for Research and Development in Chinese Medicine, State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China
³ Jiangzhong Pharmaceutical Co. Ltd., Nanchang 330049, Jiangxi, China
⁴ Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

Received:2023-11-05 Revised:2023-12-10 Accepted:2024-01-12 Online:2024-05-31 Published:2024-05-31
Contact: Liangshan Ming
About author:
^# Zhe Li and Yanlin Xiao contributed equally to this work.
Supported by:
National Natural Science Foundation of China (Grant No. 82003953, 82360777), China Postdoctoral Science Foundation (Grant No. 2019M662278), National Natural Science Foundation of Jiangxi Province (Grant No. 20202BAB216039, 20232ACB216015, 20212BAB216009 and 20232BAB206166), 2020-2022 Young Talents Support Project of Chinese Society of Chinese Medicine (Grant No. 2020-QNRC2-07), Jiangxi University of Chinese Medicine Science and Technology Innovation Team Development Program (Grant No. CXTD-22004), and Doctoral Research start-up Fund Project of Jiangxi University of Chinese Medicine (Grant No. 2021BSZR015, 2022BSZR003).

Abstract

Abstract:

Xiao Er Xi Shi formulation powder (XEXS) is often used to treat indigestion for children and its extract powders have poor functional properties. In order to prepare XEXS-PCPs (porous core-shell composite particles) with optimal properties, the central composite design was used to optimize the formulation parameters that affect the direct compaction (DC) properties of PCPs based on XEXS. The proportions of shell material and pore-forming agent were taken as independent variables, and the yield, flowability, compactibility and disintegration time of PCPs were used as the response values. It was found that the best proportions of NH₄HCO₃ and PVP K30 were 4.76% and 9.42%, respectively. Furthermore, the measured values of yield, flowability, compactibility and disintegration time were 62.00%, 38.50°, 4.02 MPa and 14.33 min, respectively. The prediction errors were 2.99%, 1.09%, 5.70 % and 2.28%, respectively. In the present study, the optimal PCPs were mixed with four DC-grade excipients for continuous DC. The results showed that the optimal PCPs had excellent DC properties and applicability. It provides ideas and theoretical support for preparing PCPs and realizing DC for other traditional Chinese medicine.

Key words: Porous core-shell composite particles, Optimization, Spray drying, Direct compaction, Application

Supporting:

Zhe Li, Yanlin Xiao, Lin Zhu, Wenjun Liu, Lingyu Yang, Zhengji Jin, Abid Naeem, Weifeng Zhu, Yi Feng, Liangshan Ming. Optimization and application of porous core-shell particles for direct compaction[J]. Journal of Chinese Pharmaceutical Sciences, 2024, 33(5): 412-429.

Figures/Tables 19

Table 1. 23 Central composite design of experiment.

Table 2. The central composite design plan and results.

Table 3. Statistical summary of Y1.

Table 4. Statistical summary of Y2.

Table 5. Powder flowability evaluation and corresponding AR.

Table 6. Statistical summary of Y3.

Table 7. Statistical summary of Y4.

Table 8. Validation results of optimized response values.

Table 9. The application of the mixture of the optimal PCPs-X-P-NH4 and DC-grade excipient for continuous DC.

References 53

[1]	Hansen, J.; Kleinebudde, P. Enabling the direct compression of metformin hydrochloride through QESD crystallization. Int. J. Pharm. 2021, 605, 120796.
[2]	Van Snick, B.; Holman, J.; Cunningham, C.; Kumar, A.; Vercruysse, J.; De Beer, T.; Remon, J.P.; Vervaet, C. Continuous direct compression as manufacturing platform for sustained release tablets. Int. J. Pharm. 2017, 519, 390–407.
[3]	Lyytikäinen, J.; Stasiak, P.; Kubelka, T.; Olenius, T.; Korhonen, O.; Ketolainen, J.; Ervasti, T. Parameter optimization in a continuous direct compression process of commercially batch-produced bisoprolol tablets. Int. J. Pharm. 2022, 628, 122355.
[4]	Zhao, H.Y.; Zhao, L.J.; Lin, X.; Shen, L. An update on microcrystalline cellulose in direct compression: functionality, critical material attributes, and co-processed excipients. Carbohydr. Polym. 2022, 278, 118968.
[5]	Kamyar, R.; Lauri Pla, D.; Husain, A.; Cogoni, G.; Wang, Z.L. Soft sensor for real-time estimation of tablet potency in continuous direct compression manufacturing operation. Int. J. Pharm. 2021, 602, 120624.
[6]	Mura, P.; Valleri, M.; Baldanzi, S.; Mennini, N. Characterization and evaluation of the performance of different calcium and magnesium salts as excipients for direct compression. Int. J. Pharm. 2019, 567, 118454.
[7]	Shah, U.V.; Karde, V.; Ghoroi, C.; Heng, J.Y.Y. Influence of particle properties on powder bulk behaviour and processability. Int. J. Pharm. 2017, 518, 138–154.
[8]	Li, Z.; Xian, J.C.; Wu, F.; Lin, X.; Shen, L.; Feng, Y. Development of TCM-based composite particles for direct compaction by particle design. Powder Technol. 2018, 338, 481–492.
[9]	Dhondt, J.; Bertels, J.; Kumar, A.; Van Hauwermeiren, D.; Ryckaert, A.; Van Snick, B.; Klingeleers, D.; Vervaet, C.; De Beer, T. A multivariate formulation and process development platform for direct compression. Int. J. Pharm. 2022, 623, 121962.
[10]	Li, Z.; Zhou, M.M.; Wu, F.; Shen, L.; Lin, X.A.; Feng, Y. Direct compaction properties of Zingiberis Rhizoma extracted powders coated with various shell materials: improvements and mechanism analysis. Int. J. Pharm. 2019, 564, 10–21.
[11]	Chen, H.B.; Wang, C.G.; Kang, H.; Zhi, B.; Haynes, C.L.; Aburub, A.; Sun, C.C. Microstructures and pharmaceutical properties of ferulic acid agglomerates prepared by different spherical crystallization methods. Int. J. Pharm. 2020, 574, 118914.
[12]	Marasini, N.; Sheikh, Z.; Wong, C.Y.J.; Hosseini, M.; Spicer, P.T.; Young, P.; Ong, H.X.; Traini, D. Development of excipients free inhalable co-spray-dried tobramycin and diclofenac formulations for cystic fibrosis using two and three fluid nozzles. Int. J. Pharm. 2022, 624, 121989.
[13]	McDonagh, A.F.; Duff, B.; Brennan, L.; Tajber, L. The impact of the degree of intimate mixing on the compaction properties of materials produced by crystallo-co-spray drying. Eur. J. Pharm. Sci. 2020, 154, 105505.
[14]	Li, Z.; Lin, X.; Shen, L.; Hong, Y.L.; Feng, Y. Composite particles based on particle engineering for direct compaction. Int. J. Pharm. 2017, 519, 272–286.
[15]	Matos, R.L.; Lu, T.J.; Prosapio, V.; McConville, C.; Leeke, G.; Ingram, A. Coprecipitation of curcumin/PVP with enhanced dissolution properties by the supercritical antisolvent process. J. CO2 Util. 2019, 30, 48–62.
[16]	Wang, C.; Liu, D.Y.; Ma, J.L.; Liang, C.; Chen, X.P. Characterization of coating shells in a Wurster fluidized bed under different drying conditions and solution viscosities. Powder Technol. 2022, 411, 117914.
[17]	Sheng, F.; Chow, P.S.; Hu, J.; Cheng, S.Y.; Guo, L.F.; Dong, Y.C. Preparation of quercetin nanorod/microcrystalline cellulose formulation via fluid bed coating crystallization for dissolution enhancement. Int. J. Pharm. 2020, 576, 118983.
[18]	Siow, C.R.S.; Tang, D.S.; Heng, P.W.S.; Chan, L.W. Probing the impact of HPMC viscosity grade and proportion on the physical properties of co-freeze-dried mannitol-HPMC tableting excipients using multivariate analysis methods. Int. J. Pharm. 2019, 556, 246–262.
[19]	Zhang, J.; Liu, M.Z.; Zeng, Z.H. The antisolvent coprecipitation method for enhanced bioavailability of poorly water-soluble drugs. Int. J. Pharm. 2022, 626, 122043.
[20]	Kolář, J.; Kovačík, P.; Choděrová, T.; Grof, Z.; Štěpánek, F. Optimization of Wurster fluid bed coating: mathematical model validated against pharmaceutical production data. Powder Technol. 2021, 386, 505–518.
[21]	Abla, K.K.; Mehanna, M.M. Freeze-drying: a flourishing strategy to fabricate stable pharmaceutical and biological products. Int. J. Pharm. 2022, 628, 122233.
[22]	Davis, M.T.; Potter, C.B.; Walker, G.M. Downstream processing of a ternary amorphous solid dispersion: the impacts of spray drying and hot melt extrusion on powder flow, compression and dissolution. Int. J. Pharm. 2018, 544, 242–253.
[23]	Bazaria, B.; Kumar, P. Optimization of spray drying parameters for beetroot juice powder using response surface methodology (RSM). J. Saudi Soc. Agric. Sci. 2018, 17, 408–415.
[24]	Tontul, I.; Topuz, A. Spray-drying of fruit and vegetable juices: effect of drying conditions on the product yield and physical properties. Trends Food Sci. Technol. 2017, 63, 91–102.
[25]	Nimbkar, S.; Leena, M.M.; Moses, J.A.; Anandharamakrishnan, C. Development of iron-vitamin multilayer encapsulates using 3 fluid nozzle spray drying. Food Chem. 2023, 406, 135035.
[26]	Funk, N.L.; Fantaus, S.; Beck, R.C.R. Immediate release 3D printed oral dosage forms: how different polymers have been explored to reach suitable drug release behaviour. Int. J. Pharm. 2022, 625, 122066.
[27]	Wazalwar, R.; Tripathi, N.; Raichur, A.M. Mechanical and curing behavior of epoxy composites reinforced with polystyrene-graphene oxide (PS-GO) core-shell particles. Compos. C. 2021, 5, 100128.
[28]	Li, J.Z.; Li, Z.; Ruan, H.S.; Gao, Y.T.; Hong, Y.L.; Shen, L.; Lin, X.A. Improved direct compression properties of Gardeniae fructus water extract powders via fluid bed-mediated surface engineering. Pharm. Dev. Technol. 2022, 27, 725–739.
[29]	Wang, H.N.; Tian, W.N.; Li, Y.; Yuan, Y.; Lv, M.W.; Cao, Y.; Xiao, J. Intervention effects of multilayer core-shell particles on colitis amelioration mechanisms of capsaicin. J. Control. Release. 2022, 351, 324–340.
[30]	Zhu, W.F.; Zhu, L.; Li, Z.; Wu, W.T.; Guan, Y.M.; Chen, L.H.; Mao, Z.X.; Ming, L.S. The novel use of PVP K30 as templating agent in production of porous lactose. Pharmaceutics. 2021, 13, 814.
[31]	Deng, K.M.; Zhang, X.Y.; Yuan, B.; Deng, Z.W.; Liu, X.; Shang, B. Porous structure with stable superhydrophobic surface for high-performance atmospheric fog harvesting. J. Environ. Chem. Eng. 2022, 10, 108771.
[32]	Dai, S.Y.; Xu, B.; Zhang, Z.Q.; Yu, J.Q.; Wang, F.; Shi, X.Y.; Qiao, Y.J. A compression behavior classification system of pharmaceutical powders for accelerating direct compression tablet formulation design. Int. J. Pharm. 2019, 572, 118742.
[33]	González, K.; Larraza, I.; Berra, G.; Eceiza, A.; Gabilondo, N. 3D printing of customized all-starch tablets with combined release kinetics. Int. J. Pharm. 2022, 622, 121872.
[34]	Ghosh Dastidar, D.; Saha, S.; Chowdhury, M. Porous microspheres: synthesis, characterisation and applications in pharmaceutical & medical fields. Int. J. Pharm. 2018, 548, 34–48.
[35]	Craparo, E.F.; Cabibbo, M.; Emanuele Drago, S.; Casula, L.; Lai, F.; Cavallaro, G. Inhalable polymeric microparticles as pharmaceutical porous powder for drug administration. Int. J. Pharm. 2022, 628, 122325.
[36]	Liao, Q.Y.; Yip, L.; Chow, M.Y.T.; Chow, S.F.; Chan, H.K.; Kwok, P.C.L.; Lam, J.K.W. Porous and highly dispersible voriconazole dry powders produced by spray freeze drying for pulmonary delivery with efficient lung deposition. Int. J. Pharm. 2019, 560, 144–154.
[37]	Li, Z.; Zhu, L.; Chen, F.C.; Guan, Y.M.; Chen, L.H.; Zhang, J.W.; Mao, Z.X.; Ming, L.S.; Zhu, W.F. The preparation, characterization, and application of porous core–shell composite particles produced with laboratory-scale spray dryer. Drug Dev. Ind. Pharm. 2023, 49, 217–231.
[38]	Vickovic, D.; Czaja, T.P.; Gaiani, C.; Pedersen, S.J.; Ahrné, L.; Hougaard, A.B. The effect of feed formulation on surface composition of powders and wall deposition during spray drying of acidified dairy products. Powder Technol. 2023, 418, 118297.
[39]	Francia, V.; Martín, L.; Bayly, A.E.; Simmons, M.J.H. Agglomeration during spray drying: airborne clusters or breakage at the walls? Chem. Eng. Sci. 2017, 162, 284–299.
[40]	Siow, C.R.S.; Heng, P.W.S.; Chan, L.W. A study on the impact of HPMC viscosity grade and proportion on the functional properties of co-freeze-dried mannitol-HPMC cushioning excipients for compacted MUPS. Eur. J. Pharm. Biopharm. 2020, 151, 98–107.
[41]	Foppoli, A.; Maroni, A.; Palugan, L.; Zema, L.; Moutaharrik, S.; Melocchi, A.; Cerea, M.; Gazzaniga, A. Erodible coatings based on HPMC and cellulase for oral time-controlled release of drugs. Int. J. Pharm. 2020, 585, 119425.
[42]	Chen, L.; Tang, Y.F.; Zhao, K.; Zha, X.; Liu, J.X.; Bai, H.; Wu, Z.X. Fabrication of the antibiotic-releasing gelatin/PMMA bone cement. Colloids Surf. B 2019, 183, 110448.
[43]	Mokeem, L.S.; Garcia, I.M.; Shahkarami, Y.; Blum, L.; Balhaddad, A.A.; Collares, F.M.; Williams, M.A.; Weir, M.D.; Melo, M.A.S. Core-shell nanostructures for improving dental restorative materials: a scoping review of composition, methods, and outcome. Smart Mater. Med. 2023, 4, 102–110.
[44]	Peng, Q.H.; Cong, H.L.; Yu, B.; Wei, L.; Mahmood, K.; Yuan, H.; Yang, R.X.; Zhang, X.Y.; Wu, Y. Preparation of polymeric Janus microparticles with hierarchically porous structure and enhanced anisotropy. J. Colloid Interface Sci. 2018, 522, 144–150.
[45]	Xiao, P.F.; Qi, P.; Chen, J.; Song, Z.L.; Wang, Y.D.; He, H.B.; Tang, X.; Wang, P.X. The effect of polymer blends on initial release regulation and in vitro-in vivo relationship of peptides loaded PLGA-Hydrogel Microspheres. Int. J. Pharm. 2020, 591, 119964.
[46]	Chaerunisaa, A.Y.; Ali, R.; Körber, M.; Bodmeier, R. Quantification of porogen effect on the drug release from single- and multi-layered ethylcellulose coated pellets containing single or combined drugs. Int. J. Pharm. 2020, 577, 119050.
[47]	Yohannes, B.; Abebe, A. Determination of tensile strength of shaped tablets. Powder Technol. 2021, 383, 11–18.
[48]	Al-Shdefat, R.; Anwer, M.K.; Fayed, M.H.; Alsulays, B.B.; Tawfeek, H.M.; Abdel-Rahman, R.F.; Soliman, G.A. Preparation and evaluation of spray dried rosuvastatin calcium-PVP microparticles for the improvement of serum lipid profile. J. Drug Deliv. Sci. Technol. 2020, 55, 101342.
[49]	Ziffels, S.; Steckel, H. Influence of amorphous content on compaction behaviour of anhydrous α-lactose. Int. J. Pharm. 2010, 387, 71–78.
[50]	Zhao, H.Y.; Shi, C.T.; Zhao, L.J.; Wang, Y.J.; Shen, L. Influences of different microcrystalline cellulose (MCC) grades on tablet quality and compression behavior of MCC-lactose binary mixtures. J. Drug Deliv. Sci. Technol. 2022, 77, 103893.
[51]	Zhang, R.H.; Pang, X.Y.; Lu, J.; Liu, L.; Zhang, S.W.; Lv, J.P. Effect of high intensity ultrasound pretreatment on functional and structural properties of micellar casein concentrates. Ultrason. Sonochem. 2018, 47, 10–16.
[52]	Ross, M.M.; Crowley, S.V.; Kelly, A.L. Applications of micellar casein concentrate in 3D-printed food structures. Innov. Food Sci. Emerg. Technol. 2022, 82, 103182.
[53]	Prikeržnik, M.; Srčič, S. Multivariate analysis for optimization and validation of the industrial tablet-manufacturing process. Drug Dev. Ind. Pharm. 2021, 47, 61–71.

Optimization and application of porous core-shell particles for direct compaction

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