Assessing compatibility of excipients selected for a sustained release formulation of bilberry leaf extract
DOI:
https://doi.org/10.1590/s2175-97902022e19753%20%20Keywords:
Bilberry leaves, Herbal extract, Thermogravimetric analysis, FTIR spectroscopy, Compatibility study, Pearson correlation analysisAbstract
The study is aimed to assess the compatibility of bilberry leaf powder extract (BLPE) with six excipients selected for sustained-release (SR) tablet formulation. The BLPE was obtained with the addition of L-arginine and Myo-inositol as the carriers. Thermogravimetric (TG-DTG) analysis and Fourier-transform infrared spectroscopy (FTIR), supported by Pearson correlation analysis, were applied to detect possible interactions in the binary mixtures (1:1) of the BLPE with each excipient. The TG-DTG showed some deviations in the thermal behavior of the BLPE / excipient mixtures. However, only the thermal behavior of magnesium stearate in the mixture significantly differed from individual samples, which suggested chemical interaction for this excipient. The FTIR analysis confirmed that the BLPE is compatible with Eudragit L100, Methocel K4M, Methocel K100LV, Avicel PH-101, and Plasdone S-630. Whereas it undergoes solid-state chemical interaction in the binary mixture with magnesium stearate. According to the FTIR-spectra, it is suggested that this interaction results in the formation of stearic acid and alkalization of the medium. These findings evidence for the possibility of using TG-DTG analysis as an independent thermal technique for compatibility studies and also confirm the earlier reported interaction of basic lubricants, e.g., stearic salts, with active ingredients containing amino groups.
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Alves R, Reis TVdS, Cides da Silva LC, Storpirtis S, Mercuri LP, Matos JdR. Thermal behavior and decomposition kinetics of rifampicin polymorphs under isothermal and non-isothermal conditions. Braz J Pharm Sci. 2010;46(2):343-351.
Araújo AAS, Mercuri LP, Seixas SRS, Storpirtis S, do Rosário Matos J. Determinação dos teores de umidade e cinzas de amostras comerciais de guaraná utilizando métodos convencionais e análise térmica [Determination of humidity and ash content of guarana commercial samples using conventional method and thermal analysis]. Rev Bras Cienc Farm. 2006;42(2):269-277. Portuguese.
Bilia A, Isacchi B, Righeschi C, Guccione C, Bergonzi MC. Flavonoids Loaded in Nanocarriers: An Opportunity to Increase Oral Bioavailability and Bioefficacy. Food Nutr Sci. 2014;5(13):1212-1327.
Bljajić K, Petlevski R, Vujić L, Čačić A, Šoštarić N, Jablan J, et al. Chemical Composition, Antioxidant and α-Glucosidase-Inhibiting Activities of the Aqueous and Hydroethanolic Extracts of Vaccinium myrtillus Leaves. Molecules. 2017;22:E703.
Castello RA, Mattocks AM. Discoloration of Tablets Containing Amines and Lactose. J Pharm Sci. 1962;51:106-108.
Cignarella A, Nastasi M, Cavalli E, Puglisi L. Novel lipid-lowering properties of Vaccinium myrtillus L. leaves, a traditional antidiabetic treatment, in several models of rat dyslipidaemia: a comparison with ciprofibrate. Thromb Res. 1996;84(5):311-322.
Conte R, Marturano V, Peluso G, Calarco A, Cerruti P. Recent Advances in Nanoparticle-Mediated Delivery of Anti-Inflammatory Phytocompounds. Int J Mol Sci. 2017;18(4):E709.
Council of Europe. European pharmacopoeia, 9th ed. Strasbourg: Council of Europe; 2016.
Da Silva EP, Pereira MAV, De Barros Lima IP, Lima NGPB, Barbosa EG, Aragão CFS, et al. Compatibility study between atorvastatin and excipients using DSC and FTIR. J Therm Anal Calorim. 2016;123:933-939.
De Barros Lima IP, Lima NGPB, Barros DMC, Oliveira TS, Barbosa EG, Gomes APB, et al. Compatibility study of tretinoin with several pharmaceutical excipients by thermal and non-thermal techniques. J Therm Anal Calorim . 2015;120:733-747.
Disch L, Forsch K, Siewert B, Drewe J, Fricker G. Sustained Release for St. John’s Wort: A Rational Idea? J Bioequiv Bioavailab. 2017;9(6):565-576.
Gallo L, Piña J, Bucalá V, Allemandi D, Ramírez-Rigo MV. Development of a modified-release hydrophilic matrix system of a plant extract based on co-spray-dried powders. Powder Technol. 2013;241:252-262.
Hotha KK, Roychowdhury S, Subramanian V. Drug-Excipient Interactions: Case Studies and Overview of Drug Degradation Pathways. Am J Anal Chem. 2016;7(1):107-140.
Jones TM. Preformulation Studies. In: Tovey GD, editor. Pharmaceutical Formulation: The Science and Technology of Dosage Forms. Croydon: The Royal Society of Chemistry; 2018, p. 1-41.
Kararli TT, Needham TE, Seul CJ, Finnegan PM. Solid-state interaction of magnesium oxide and ibuprofen to form a salt. Pharm Res. 1989;6:804-808.
Koshovyi OM, Zagayko AL, Kolychev IO, Akhmedov EYu, Komissarenko AN. [Phytochemical study of the dry extract from bilberry leaves]. Azerbaijan Pharm. Pharmacother. J. 2016a;16(1):18-23. Russian.
Koshovyi OM, Zagayko AL, Kolychev IO, Fylymonenko VP, Komisarenko AM, inventors; National University of Pharmacy, assignee. Method for producing hypoglycemic composition from leaves of blueberry (Vaccinium myrtillus L.). UA patent 111134. March 25, 2016b. Ukrainian.
Lavor EP, Navarro MVM, Freire FD, Aragão CFS, Raffin FN, Barbosa EG, et al. Application of thermal analysis to the study of antituberculosis drugs-excipient compatibility. J Therm Anal Calorim . 2014;115:2303-2309.
Li J, Wu Y. Lubricants in Pharmaceutical Solid Dosage Forms. Lubricants. 2014;2(1):21-43.
Liltorp K, Larsen TG, Willumsen B, Holm R: Solid state compatibility studies with tablet excipients using non thermal methods. J Pharm Biomed Anal. 2011;55(3):424-428.
Maderuelo C, Zarzuelo A, Lanao JM. Critical factors in the release of drugs from sustained release hydrophilic matrices. J Control Release. 2011;154(1):2-19.
Mainardes RM, Gremião MPD, Evangelista RC. Thermoanalytical study of praziquantel-loaded PLGA nanoparticles. Rev Bras Cienc Farm . 2006;42(4):523-530.
Mancini S, Nardo L, Gregori M, Ribeiro I, Mantegazza F, Delerue-Matos C, et al. Functionalized liposomes and phytosomes loading Annona muricata L. aqueous extract: Potential nanoshuttles for brain-delivery of phenolic compounds. Phytomedicine. 2018;42:233-244.
Mishra DP, Srivastava A, Shukla RK. Spectroscopic and chemical reactivity analysis of D-Myo-Inositol using quantum chemical approach and its experimental verification. Pramana. 2017;89:12.
Monajjemzadeh F, Ghaderi F. Thermal Analysis Methods in Pharmaceutical Quality Control. J Mol Pharm Org Process Res. 2015;3(1):e121.
Mouhid L, Corzo-Martínez M, Torres C, Vázquez L, Reglero G, Fornari T, et al. Improving In Vivo Efficacy of BioactiveMolecules : An Overview of Potentially Antitumor Phytochemicals and Currently Available Lipid-Based Delivery Systems. J Oncol. 2017;2017(12):7351976.
Nestby R, Percival D, Martinussen I, Opstad N, Rohloff J. The European blueberry (Vaccinium myrtillus L.) and the potential for cultivation. A review. Eur J Plant Sci Biotechnol. 2011;5:5-16.
Neto HS, Novák Cs, Matos JR. Thermal analysis and compatibility studies of prednicarbate with excipients used in semi solid pharmaceutical form. J Therm Anal Calorim . 2009;97(1):367-374.
Pramod K, Suneesh CV, Shanavas S, Ansari SH, Ali J. Unveiling the compatibility of eugenol with formulation excipients by systematic drug-excipient compatibility studies. J Anal Sci Technol. 2015;6(1):34.
Ramešová Š, Sokolová R, Degano I, Bulíčková J, Žabka J, Gál M. On the stability of the bioactive flavonoids quercetin and luteolin under oxygen-free conditions. Anal Bioanal Chem. 2012;402(2):975-982.
Santana CP, Fernandes FHA, Brandão DO, Silva PCD, Correia LP, Nóbrega FP, et al. Compatibility study of dry extract of Ximenia americana L. and pharmaceutical excipients used in solid state. J Therm Anal Calorim . 2018;133:603-617.
Sidorova Y, Shipelin V, Mazo V, Zorin S, Petrov N, Kochetkova A. Hypoglycemic and hypolipidemic effect of Vaccinium myrtillus L. leaf and Phaseolus vulgaris L. seed coat extracts in diabetic rats. Nutrition. 2017;41:107-112.
Silverstein RM, Webster FX, Kiemle DJ. Spectrometric identification of organic compounds. 7th ed. Hoboken (NJ): John Wiley & Sons, Inc.; 2005.
Singhal A, Jain H, Singhal V, Elias EJ, Showkat A. Colon-targeted quercetin delivery using natural polymer to enhance its bioavailability. Pharmacogn Res. 2011;3(1):35-39.
Suvarna V, Gujar P, Murahari M. Complexation of phytochemicals with cyclodextrin derivatives - An insight. Biomed Pharmacother. 2017;88:1122-1144.
Talvani A, Bahia MT, de Sá-Barreto LCL, Lima EM, da Cunha-Filho MSS. Carvedilol: decomposition kinetics and compatibility with pharmaceutical excipients. J Therm Anal Calorim . 2014;115:2501-2506.
Wesolowski M, Rojek B. Thermogravimetric detection of incompatibilities between atenolol and excipients using multivariate techniques. J Therm Anal Calorim . 2013;113:169-177.
Zagayko AL, Kolisnyk TYe, Chumak OI, Ruban OA, Koshovyi OM. Evaluation of anti-obesity and lipid-lowering properties of Vaccinium myrtillus leaves powder extract in a hamster model. J Basic Clin Physiol Pharmacol. 2018;29(6):697-703.
Ziegler-Borowska M, Chełminiak D, Kaczmarek H. Thermal stability of magnetic nanoparticles coated by blends of modified chitosan and poly(quaternary ammonium) salt. J Therm Anal Calorim . 2015;119:499-506.
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