Effect of carrier materials on the properties of the andrographolide solid dispersion
DOI:
https://doi.org/10.1590/s2175-97902022e191023%20%20Keywords:
Andrographolide, Solid dispersion, Physicochemical properties, DissolutionAbstract
n the work the andrographolide (AG)-solid dispersions (SDs) were prepared by the spray-drying method, using polyethylene glycol 8000 (PEG8000), Poloxamer188, polyvinylpyrrolidone K30 (PVPK30), Soluplus® as carrier materials. The effect of different polymers as carrier materials on the properties of the AG-SDs were studied. The results showed obvious differences in intermolecular interaction, thermal stability, drug state, powder properties, dissolution behavior, and so on of AG-SDs prepared using different polymers as carrier materials. AG-PEG8000-SD was a partial-crystalline and partial-amorphous powder with smaller surface area and pore volume, but it was easy to wetting and did not swell in contact with dissolved medium. AG-Soluplus®-SD was completely amorphous powder with larger specific surface area and pore volume, but it swelled in contact with water. Therefore, the dissolution profile of AG in AG-PEG8000-SD was similar to that in AG-Soluplus®-SD. Soluplus® and PEG8000 were suitable polymers to design AG-SDs, considering both physicochemical properties and dissolution behaviors. The results of this reseach showed that when selecting carrier materials for SD, we should not only consider the state of drugs in SD and the powder properties of SD, but also consider whether there is swelling when the carrier materials are in contact with the dissolution medium.
Downloads
References
Albadarin AB, Potter CB, Davis MT, Iqbal J, Korde S, Pagire S, et al. Development of stability-enhanced ternary solid dispersions via combinations of HPMCP and Soluplus® processed by hot melt extrusion. Int J Pharm. 2017;532(1):603-11.
Barmpalexis P, Koutsidis I, Karavas E, Louka D, Papadimitriou SA, Bikiaris DN. Development of PVP/PEG mixtures as appropriate carriers for the preparation of drug solid dispersions by melt mixing technique and optimization of dissolution using artificial neural networks. Eur J Pharm Biopharm. 2013;85(3):1219-31.
Bhardwaj V, Trasi NS, Zemlyanov DY, Taylor LS. Surface area normalized dissolution to study differences in itraconazole-copovidone solid dispersions prepared by spray-drying and hot melt extrusion. Int J Pharm . 2018;540(1-2):106-19.
Bikiaris D, Papageorgiou GZ, Stergiou A, Pavlidou E, Karavas E, Kanaze F, et al. Physicochemical studies on solid dispersions of poorly water-soluble drugs - Evaluation of capabilities and limitations of thermal analysis techniques. Thermochim Acta. 2005;439(1-2):58-67.
Bothiraja C, Shinde MB, Rajalakshmi S, Pawar AP. Evaluation of molecular pharmaceutical and in-vivo properties of spray-dried isolated andrographolide-PVP. J Pharm Pharmacol. 2009;61(11):1465-72.
Calabrese C, Berman SH, Babish JG, Ma X, Shinto L, Dorr M, et al. A phase I trial of andrographolide in HIV positive patients and normal volunteers. Phytother Res. 2000;14(5):333-8.
Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci. 1971;60(9):1281-302.
Chokshi RJ, Zia H, Sandhu HK, Shah NH, Malick WA. Improving the dissolution rate of poorly water soluble drug by solid dispersion and solid solution: pros and cons. Drug Deliv. 2007;14(1): 33-45.
Chutimaworapan S, Ritthidej GC, Yonemochi E, Oguchi T, Yamamoto K. Effect of water-soluble carriers on dissolution characteristics of nifedipine solid dispersions. Drug Dev Ind Pharm. 2000;26(11):1141-50.
Eloy JO, Marchetti JM. Solid dispersions containing ursolic acid in Poloxamer 407 and PEG 6000: A comparative study of fusion and solvent methods. Powder Technol. 2014;253:98-106.
FDA. Waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a biopharmaceutics classification system. Guidance for Industry. 2000.
Hu XY, Lou H, Hageman MJ. Preparation of lapatinib ditosylate solid dispersions using solvent rotary evaporation and hot melt extrusion for solubility and dissolution enhancement. Int J Pharm . 2018;552(1-2):154-63.
Jiang Y, Wang F, Xu H, Liu H, Meng Q, Liu W. Development of andrographolide loaded PLGA microspheres: optimization, characterization and in vitro-in vivo correlation. Int J Pharm . 2014;475(1-2):475-84.
Kawabata Y, Wada K, Nakatani M, Yamada S, Onoue S. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications. Int J Pharm . 2011;420(1):1-10.
Lim RTY, Ng WK, Tan RBH. Dissolution enhancement of indomethacin via amorphization using co-milling and supercritical co-precipitation processing. Powder Technol . 2013;240:79-87.
Mahmah O, Tabbakh R, Kelly A, Paradkar A. A comparative study of the effect of spray drying and hot-melt extrusion on the properties of amorphous solid dispersions containing felodipine. J Pharm Pharmacol . 2014;66(2):275-84.
Marasini N, Tran TH, Poudel BK, Cho HJ, Choi YK, Chi SC, et al. Fabrication and evaluation of pH-modulated solid dispersion for telmisartan by spray-drying technique. Int J Pharm . 2013;441(1-2):424-32.
Matsuda T, Kuroyanagi M, Sugiyama S, Umehara K, Ueno A, Nishi K. Cell differentiation-inducing diterpenes from Andrographis paniculata Nees. Chem Pharm Bull (Tokyo). 1994;42(6):1216-25.
Mohammadi G, Barzegar-Jalali M, Valizadeh H, Nazemiyeh H, Barzegar-Jalali A, Siahi Shadbad MR, et al. Reciprocal powered time model for release kinetic analysis of ibuprofen solid dispersions in oleaster powder, microcrystalline cellulose and crospovidone. J Pharm Pharm Sci. 2010;13(2):152-61.
Ramadhani N, Shabir M, McConville C. Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram. Int J Pharm . 2014;475(1-2):514-22.
Reginald-Opara JN, Attama A, Ofokansi K, Umeyor C, Kenechukwu. Molecular interaction between glimepiride and Soluplus(R)-PEG 4000 hybrid based solid dispersions: characterisation and anti-diabetic studies. Int J Pharm . 2015;496(2):741-750.
Sermkaew N, Ketjinda W, Boonme P, Phadoongsombut N, Wiwattanapatapee R. Liquid and solid self-microemulsifying drug delivery systems for improving the oral bioavailability of andrographolide from a crude extract of Andrographis paniculata. Eur J Pharm Sci . 2013;50(3-4):459-66.
Shen YC, Chen CF, Chiou WF. Andrographolide prevents oxygen radical production by human neutrophils: possible mechanism(s) involved in its anti-inflammatory effect. Br J Pharmacol. 2002;135(2):399-406.
Shi NQ, Lei YS, Song LM, Yao J, Zhang XB, Wang XL. Impact of amorphous and semicrystalline polymers on the dissolution and crystallization inhibition of pioglitazone solid dispersions. Powder Technol . 2013;247:211-21.
Singha PK, Roy S, Dey S. Protective activity of andrographolide and arabinogalactan proteins from Andrographis paniculata Nees. against ethanol-induced toxicity in mice. J Ethnopharmacol. 2007;111(1):13-21.
Singh G, Kaur L, Gupta GD, Sharma S. Enhancement of the solubility of poorly water soluble drugs through solid dispersion: a comprehensive review. Indian J Pharm Sci . 2017;79(5):674-87.
Sousa JJ, Sousa A, Podczeck F, Newton JM. Factors influencing the physical characteristics of pellets obtained by extrusion-spheronization. Int J Pharm . 2002;232(1-2):91-106.
Thenmozhi K, Yoo YJ. Enhanced solubility of piperine using hydrophilic carrier-based potent solid dispersion systems. Drug Dev Ind Pharm . 2017;43(9):1501-9.
Thybo P, Pedersen BL, Hovgaard L, Holm R, Mullertz A. Characterization and physical stability of spray dried solid dispersions of probucol and PVP-K30. Pharm Dev Technol. 2008;13(5):375-86.
Thiry J, Lebrun P, Vinassa C, Adam M, Netchacovitch L, Ziemons E, et al. Continuous production of itraconazole-based solid dispersions by hot melt extrusion: Preformulation, optimization and design space determination. Int J Pharm . 2016;515(1-2):114-24.
Veronez IP, Daniel JSP, Júnior CEC, Garcia JS, Trevisan MG. Development, characterization, and stability studies of ethinyl estradiol solid dispersion. J Therm Anal Calorim. 2015;120(1):573-81.
Vo CL, Park C, Lee BJ. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm . 2013;85(3 Pt B):799-813.
Wen L, Xia N, Chen X, Li Y, Hong Y, Liu Y, et al. Activity of antibacterial, antiviral, anti-inflammatory in compounds andrographolide salt. Eur J Pharmacol. 2014;740:421-7.
Zhang XF, Tan BK. Antihyperglycaemic and anti-oxidant properties of Andrographis paniculata in normal and diabetic rats. Clin Exp Pharmacol Physiol. 2000;27(5-6):358-63.
Zhang Y, Hu X, Liu X, Dandan Y, Di D, Yin T, et al. Dry state microcrystals stabilized by an HPMC film to improve the bioavailability of andrographolide. Int J Pharm . 2015;493(1-2):214-23.
Zhao GW, Zeng QY, Zhang SD, Zhong YQ, Wang CH, Chen YS, et al. Effect of carrier lipophilicity and preparation method on the properties of andrographolide-solid dispersion. Pharmaceutics. 2019;11(2):74-91.
Downloads
Published
Issue
Section
License
Copyright (c) 2022 Brazilian Journal of Pharmaceutical Sciences
This work is licensed under a Creative Commons Attribution 4.0 International License.
All content of the journal, except where identified, is licensed under a Creative Commons attribution-type BY.
The on line journal has open and free access.
How to Cite
Funding data
-
Jiangxi Normal University
Grant numbers GJJ201233 -
National Natural Science Foundation of China
Grant numbers 81560654
