Abstract
Purpose
Among the several therapeutic agents available for the management of diabetes mellitus, sulfonylureas such as gliclazide have several advantages. The hypoglycemic effect and bioavailability of gliclazide loaded in Isabgol husk mucilage microparticles were assessed. The hypoglycemic effect of drug-loaded microparticles was compared with that of pure gliclazide.
Methods
Gliclazide was incorporated into Isabgol husk mucilage microparticles using an emulsification-crosslinking technique. Gliclazide characterization was performed using a chromatographic method.
Results
Gliclazide loading in the microparticles was up to 91.23 ± 0.981% w/w. The pharmacokinetic parameters for pure gliclazide (control) were different from those of gliclazide loaded in microparticles (test). After oral administration, the AUC0–24 h of gliclazide in blood samples of the control and test groups was 10.840 ± 0.018 and 17.608 ± 0.035 μg/(mL h), respectively. In 24 h after oral administration, the percentage reduction from the baseline glucose level in diabetic rabbits was 36.66 ± 4.509% and 98.11 ± 1.018% for the test and control groups, respectively.
Conclusion
The prolonged hypoglycemic effect and increased bioavailability of gliclazide loaded in Isabgol husk microparticles compared with those of pure drug indicate the applicability of the microparticulate formulation as a novel anti-diabetic drug delivery system.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Abdelbary A, El-Gendy NA, Hosny A (2012) Microencapsulation approach for orally extended delivery of glipizide: in vitro and in vivo evaluation. Ind J Pharm Sci 74(4):319–330
Al-Kassas RS, Al-Gohary OMN, Al-Faadhel MM (2007) Controlling of systemic absorption of gliclazide through incorporation into alginate beads. Int J Pharm 341:230–237
Chatterjee S, Khunti K, Davies MJ (2017) Type 2 diabetes. Lancet 389(10085):2239–2251
Davis SS (1985) The design and evaluation of controlled release systems for the gastrointestinal tract. J Control Release 2:27–38
Del Guerra S, Grupillo M, Masini M, Lupi R, Bugliani M, Torri S, Boggi U, Del Chiaro M, Vistoli F, Mosca F, Del Prato S, Marchetti P (2007) Gliclazide protects human islet beta-cells from apoptosis induced by intermittent high glucose. Diabetes Metabol Res Rev 23(3):234–238
Desai A, Shidhaye S, Kadam VJ (2007) Possible use of psyllium husk as a release retardant. Ind J Pharm Sci 69(2):206–210
Devrim B, Canefe K (2006) Preparation and evaluation of modified released ibuprofen microspheres with acrylic polymers by quasi emulsion solvent diffusion method: effect of variables. Acta Pol Pharm 63:521–534
Gaur KP, Soam K, Gupta SK, Dabral P (2012) Formulation and evaluation of rifampicin sustained-release tablets using the juice of Citrus limetta as bio-retardant. J Pharm Bioallied Sci 4(Suppl 1):S25–S26
Harrower A (2000) Gliclazide modified release: from once-daily administration to 24-hour blood glucose control. Metabolism 49(10):7–11
Indian Pharmacopoeia (1996) Ministry of health and family welfare, 4th edn. Govt. of India, New Delhi
International Conference on Harmonization, Draft Guideline on Validation of Analytical Procedures (1995) Definitions and Terminology, Federal Register, 60: 11260
Kuo CY, Wu SM (2005) High-performance liquid chromatography with electrochemical detection for analysis of gliclazide in plasma. J Chromatogr A 1088:131–135
Mailhot J (1993) Efficacy and safety of gliclazide in the treatment of non-insulin dependent diabetes mellitus: a Canadian multicenter study. Clin Ther 15:1060–1068
Mi FL, Kuan CY, Shyu SS, Lee ST, Chang SF (2000) The study of gelation kinetics and chain-relaxation properties of glutaraldehyde-cross-linked chitosan gel and their effects on microspheres preparation and drug release. Carbohydr Polym 41:389–396
Nep EI, Kaur N, Shaboun S, Adebisi AO, Smith AM, Conway BR, Asare-Addo K (2020) Mechanical and release behavior of theophylline from matrix tablets containing psyllium powder in combination with Grewia polysaccharides. Colloids Surf B 188:110809
Noguchi H, Tomita N, Naruto S, Nakano D (1992) Determination of gliclazide in serum by high-performance liquid chromatography using solid-phase extraction. J Chromatogr 583(2):266–269
Nouri-Felekoria M, Khakbiza M, Nezafatib N, Mohammadia J, Eslaminejad MB (2019) Comparative analysis and properties evaluation of gelatin microspheres crosslinked with glutaraldehyde and 3-glycidoxypropyltrimethoxysilane as drug delivery systems for the antibiotic vancomycin. Int J Pharm 557:208–220
Paget GE, Barners JM (1994) Toxicity tests. In: Lurence DR, Bacharach AL (eds) Evaluation of drug activities pharmacometrics, vol 1, 34th edn. Academic Press, New York, pp 134–166
Park JY, Kim KA, Kim S-L, Park P-W (2004) Quantification of gliclazide by semi-micro high-performance liquid chromatography: application to a bioequivalence study of two formulations in healthy subjects. J Pharm Biomed Anal 35(4):943–949
Poirier JM, Perez M, Cheymol G (1987) High performance liquid chromatographic determination of gliclazide in human plasma. J Chromatogr A 421(1):223–226
Ritschel WA (1989) Biopharmaceutics and pharmacokinetic aspects in the design of controlled release peroral drug delivery systems. Drug Dev Ind Pharm 15:1073–1103
Saeedi P, Petersohn I, Salpea P, Malanda B, Karuranga S, Unwin N, Colagiuri S, Guariguata L, Motala AA, Ogurtsova K, Shaw JE, Bright D, Williams R (2019) Global and regional diabetes prevalence estimates for 2019 and projections for 2030 and 2045: results from the International Diabetes Federation Diabetes Atlas, 9th edition. Diabetes Res Clin Pract 157:107843
Senthil A, Thakkar-Hardik R, Ravikumar NVB (2011) Chitosan loaded mucoadhesive microspheres of gliclazide: in vitro and in vivo evaluation. RGUHS J Pharm Sci 1(2):163–171
Sharma VK, Bhattacharya A (2008) Release of metformin hydrochloride from Ispaghula-sodium alginate beads adhered on cock intestinal mucosa. Indian J Pharm Educ Res 42(4):363–370
Sharma VK, Mazumder B (2014a) Gastrointestinal transition and anti-diabetic effect of Isabgol husk microparticles containing gliclazide. Int J Biol Macromol 66:15–25
Sharma VK, Mazumder B (2014b) Crosslinking of Isabgol husk polysaccharides for microspheres development and its impact on particle size, swelling kinetics, and thermal behavior. Polym Bull 71:735–757
Sharma VK, Sharma PP, Mazumder B, Bhatnagar A (2015) Mucoadhesivity characterization of Isabgol husk mucilage microspheres crosslinked by glutaraldehyde. Curr Drug Del 12(6):693–702
Sujja-areevath J, Munday DL, Cox PJ, Khan KA (1996) Release characteristics of diclofenac sodium from encapsulated natural gum mini-matrix formulations. Int J Pharm 139:53–62
Timothy MED, Daly F, John PW, Kenneth FI, John PB, Leon JD (2000) Pharmacokinetics and pharmacodynamics of gliclazide in Caucasians and Australian aborigines with type-2 diabetes. J Clin Pharmacol 49:223–230
Author information
Authors and Affiliations
Corresponding author
Ethics declarations
Conflict of interest
The authors declare that they have no conflict of interest.
Statement of human and animal rights
All applicable international, national, and/or institutional guidelines for the care and use of animals were followed. All procedures performed in studies involving animals were in accordance with the ethical standards of the institution or practice at which the studies were conducted (Reg. No. 1147/ab/07/CPCSEA/2012).
Additional information
Publisher's Note
Springer Nature remains neutral with regard to jurisdictional claims in published maps and institutional affiliations.
Rights and permissions
About this article
Cite this article
Kumar, V., Mazumder, B., Sharma, P.P. et al. Pharmacokinetics and hypoglycemic effect of gliclazide loaded in Isabgol husk mucilage microparticles. J. Pharm. Investig. 51, 159–171 (2021). https://doi.org/10.1007/s40005-020-00494-9
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s40005-020-00494-9