Nanocrystal Formation of Hydrochlorothiazide: Effect of a Surfactant on the Solid-State Properties
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Abstract
Background: Modification of solid-state properties is associated with nanocrystallization of drug substances, and crucial to processability of materials during formulation. This work was aimed at assessing the effect of a surfactant on the solid-state properties in nanocrystal formation of hydrochlorothiazide.
Methods: The drug powder was subjected to two forms of nanocrystallization: with and without the inclusion of Tween 80, a surfactant. The two generated nanocrystal forms, in comparison with the unprocessed drug, were subjected to Fourier transform infrared spectroscopy, differential scanning calorimetry and particle size analysis.
Results: All the major peaks in the FTIR spectrum of hydrochlorothiazide powder (HCTZ1) were retained in the spectrum of crystals generated without the addition of Tween 80 (HCTZ2) and in that of the crystals generated with the addition of Tween 80 (HCTZ3). The thermogram of HCTZ1 showed a sharp endothermic transition with a peak at 77 0C followed by a diffuse endotherm with a peak at 235 0C; that of HCTZ2 was characterized by a diffuse endotherm with a peak at 110 0C and a diffuse exotherm with a peak at 250 0C while that of HCTZ3 was characterized by a single endotherm with a peak at 133 0C.
Conclusion: Simple nanocrystallization causes a decrease in the particle size of hydrochlorothiazide but with a disruption in the thermal properties while the inclusion of a surfactant in the nanocrystallization process causes a further decrease in the size and an improvement in the thermal behaviour of the drug.
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References
O’Neil MJ. The Merck Index- An Encyclopaedia of Chemicals, Drugs and Biologicals. Cambridge, UK: Royal Society of Chemistry; 2013. p. 885.
Yalkowsky SH, He Y, Jain P. Handbook of Aqueous Solubility Data. Second edition. Boca Raton: CRC Press; 2010. pp. 392.
Olorunsola EO, Adedokun MO, Samuel OU, Joseph MG. Effects of Prosochit binder on the dissolution and permeation of a BCS class IV drug. Trop J Nat Prod Res 2021; 5(6): 1138-1141.
Safwan A, Raghad AK, Banana A. Hydrochlorothiazide used as diuretic with antihypertensive agents in pharmaceutical preparations: Estimation by first-order derivative and extractive spectrophotometry. Can J Chem 2014; 2(2): 190-200.
Lipinski CA. Drug-like properties and the causes of poor solubility and poor permeability. J Pharmacol Toxicol Methods 2020; 44(1):235–249.
Olorunsola EO, Davies KG, Essien EB; Alozie M.F, Adedokun MO, Ahsan, F. Orally administered Prosochit®?based nanoparticles of insulin ameliorates alloxan?induced diabetes in rats. Sci Pharm 2022; 90: 66. https://doi.org/10.3390/ scipharm90040066
Gursoy RN, Benita S. Self-emulsifying-drug delivery systems (SEDDS) for improved oral delivery of lipophilic drug. Biomed Pharmacother 2004; 58: 173–182
Growthamarajan K, Sachin KS. Dissolution testing for poorly soluble drugs: A continuing perspective. Dissolution Technol 2010; 17: 24-32.
Khan A, Iqbal Z, Shah Y, Ahmad L, Ullah Z, Ullah A. Enhancement of dissolution rate of class II drugs (hydrochlorothiazide). A comparative study of the two novel approaches; solid dispersion and liquid-solid techniques. Saudi Pharm J 2015; 23: 650-657.
Cirri M, Maestrini L, Maestrelli F, Mennini N, Mura P, Ghelardini C, Mannelli LDC. Design, characterization and in vivo evaluation of nanostructured lipid carriers (NLC) as a new drug delivery system for hydrochlorothiazide oral administration in paediatric therapy. Drug Deliv 2018; 25(1): 1910-1921.
Hirlekar R, Kadam V. Preparation and characterization of inclusion complexes of carvedilol with methyl-?-cyclodextrin. J Incl Phenom Macrocycl Chem 2009; 63: 219-240.
Gao L, Zhang D, Chen M. Drug nanocrystals for the formulation of poorly soluble drugs and its application as a potential drug delivery system. J Nanopart Res 2008; 10: 845–862.
Chen H, Khemtong C, Yang X, Chang X, Gao J.Nanonization strategies for poorly water-soluble drugs. Drug Discov Today 2011; 16(7-8): 354–360.
Ajmal C, Ganesh NS, Mafibaniasadi Z, Chandy V. Nanosuspension: Promoting solubility of drugs by nanotechnology. World J Pharm Pharm Sci 2019; 8(7): 353-354.
Katteboina S, Chandrasesekhar P, Balaji S. Drug nanocrystals: A novel formulation approach for poorly soluble drugs. Int J Pharm Technol Res 2009; 1(3): 682-694.
Olorunsola EO, Davies KG, Ibiang KP, Esukpa PC, Uwaechi EG, Ahsan F. Prosochit®-based nanoparticulate system of insulin for oral delivery: design, formulation and characterization. J Appl Pharm Sci 2023; 13(03): 044–052
Yang L, Huang JM, Zu YG, Ma CH, Wang H, Sun XW, Sun Z. Preparation and radical scavenging activities of polymeric procyanidins nanoparticles by a supercritical antisolvent (SAS) process. Food Chem 2011; 128: 1152–1159.
Mokale V, Khatumaria B, Verma U, Shimpi N, Naik J, Mishra S. Formulation and development of nanoparticles for quick and complete release of hydrochlorothiazide by nanonization technique. Micro and Nanosystems 2014; 6: 109-117.
Olorunsola EO, Bhatia PG, Tytler BA, Adikwu MU. Some chemical characteristics of novel hemicellulosic gums from seeds of Afzelia africana and Prosopis africana. West Afr J Pharm 2014; 25(2) 31-40.
Phromviyo N, Swatsitang E, Chompoosor A. Effect of a surface stabilizer on the formation of polyoxalate nanoparticles and their release profiles. Vacuum 2014; 107: 208–212.
Müller RH, Gohla S, Keck CM. State of the art of nanocrystals - special features, production, nanotoxicology aspects and intracellular delivery. Eur J Pharma Biopharm 2011; 78(1): 1-9.
Olorunsola EO, Bhatia PG, Tytler BA, Adikwu MU. Thermochemical properties of hydrophilic polymers from cashew and khaya exudates and their implications on drug delivery. J Drug Deliv 2016; (7496585): 1–7. http://dx.doi.org/10.1155/2016/7496585.
Zirak MB, Pezeshki A. Effect of surfactant concentration on the particle size, stability and potential zeta of beta carotene nano lipid carrier. Int J Curr Microbiol Appl Sci 2015; 4(9): 924-932.