Optimization and characterization of xanthan gum based multiparticulate formulation for colon targeting

Abstract

To optimize and characterize xanthan gum multi-particulate formulation for colon targeting, which increases the residence time at the absorbing surface of the colon. Xanthan gum was dispersed in cold water containing drug and was permitted to expand for 2 h. Sodium alginate was blended well in 10 ml of water. Xanthan gum solution containing the drug was added to sodium alginate solution and 0.3 ml of glutaraldehyde was added to the dispersion, with constant stirring. Then, polymer-drug solution was added dropwise into 5% w/v calcium chloride solution with continuous stirring, producing microspheres filtered by Whatman filter paper and dried at 30 °C–40 °C. Microspheres were performed by chemical cross-linking with glutaraldehyde, which increased the maximum drug entrapment efficiency up to 73.63 ± 0.65% with an increasing concentration of xanthan gum polymer 0.7% w/v for the optimized F6 batch. Better results were found by increasing the polymer concentration along with the glutaraldehyde concentration. The kinetics of drug release for the F6 batch was considered as an optimized batch because the regression value was found to be 0.997 in the peppas model. The accelerated stability study on the optimized F6 batch performed to learn whether the drug has any change during its period of usability. The polysaccharide remains intact in the stomach and intestine and the drug was released in the colon with low toxicity and biodegradability. The present studies showed that optimizing and characterizing xanthan gum multiparticulate formulation for colon targeting gives metronidazole the most effective and controlled delivery.

Keywords

Microspheres / Polysaccharides / Glutaraldehyde / Biodegradability / Colon

References

[1] Lee SH, Bajracharya R, Min JY, Han JW, Park BJ, Han HK. Strategic approaches for colon targeted drug delivery: an overview of recent advancements. Pharmaceutics. 2020;12:68.

[2] Beaugerie L, Itzkowitz SH. Cancers complicating inflammatory bowel disease. N Engl J Med. 2015;372(15):1441–1445.

[3] Teruel AH, Gonzalez-Alvarez I, Bermejo M, et al. New insights of oral colonic drug delivery systems for inflammatory bowel disease therapy. Int J Mol Sci. 2020;21(18):6502.

[4] Maroni A, Zema L, Maria DDC, et al. Oral colon delivery of insulin with the aid of functional adjuvants. Adv Drug Deliv Rev. 2012;64(6):540–556.

[5] Abet V, Filace F, Recio J, Alvarez-Builla J, Burgos C. Prodrug approach: an overview of recent cases. Eur J Med Chem. 2017;127:810–827.

[6] Mazumder R, Nath LK, Haque A, et al. Formulation and in vitro evaluation of natural polymers-based microspheres for colonic drug delivery. Int J Pharm Pharmaceut Sci. 2010;2(1):211–219.

[7] Mazumder R, Mahanti B, Majumdar S, et al. Satranidazole-loaded chitosan/locust bean gum/xanthan gum polysaccharide composite multiunit pellets for colon targeting: in vitro–in vivo investigation. Beni-Suef Univ J Basic Appl Sci. 2022;11:151.

[8] Haghshenas B, et al. Microencapsulation of probiotic bacteria Lactobacillus plantarum 15 HN using alginate psyllium fenugreek polymeric blends. J Appl Microbiol. 2015;118(4):1048–1057.

[9] Agarwal T, et al. Calcium alginate-carboxymethyl cellulose beads for colon-targeted drug delivery. Int J Biol Macromol. 2015;75:409–417.

[10] Chaurasia G, et al. A review on pharmaceutical preformulation studies in formulation and development of new drug molecules. Int J Pharma Sci Res. 2016;7(6):2313.

[11] Rezvanian M, et al. Development and physicochemical characterization of alginate composite film loaded with simvastatin as a potential wound dressing. Carbohydr Polym. 2016;137:295–304.

[12] Wang H, et al. Highly enhanced visible light photo catalysis and in situ FT-IR studies on Bi metal defective BiOCl hierarchical microspheres. Appl Catal B Environ. 2018;225:218–227.

[13] Khan S, et al. Formulation and evaluation of multiparticulate gel beads containing tinidazole for stomach specific delivery. Int J Pharm Tech Res. 2015;8(8):196–205.

[14] Awasthi R. Preparation, characterization and evaluation of ranitidine hydrochlorideloaded mucoadhesive microspheres. Polim Med. 2014;44(2):75–81.

[15] Ramteke KH, et al. Preparation, evaluation and optimization of multiparticulate system of mebendazole for colon targeted drug delivery by using natural polysaccharides. Adv Pharmaceut Bull. 2015;5(3):361.

[16] Weissman SA, Anderson NG. Design of experiments (DoE) and process optimization. A review of recent publications. Org Process Res Dev. 2015;19(11):1605–1633.

[17] Beg S, et al. Solid self-nanoemulsifying systems of Olmesartan medoxomil: formulation development, micromeritic characterization, in vitro and in vivo evaluation. Powder Technol. 2016;294:93–104.

[18] Newbury DE, Ritchie NW. Performing elemental microanalysis with high accuracy and high precision by scanning electron microscopy/silicon drift detector energy-dispersive X-ray spectrometry (SEM/SDD-EDS). J Mater Sci. 2015;50(2):493–518.

[19] Abdalla KF, et al. Optimization of the entrapment efficiency and release of ambroxol hydrochloride alginate beads. J Appl Pharmaceut Sci. 2015;5(4):13–19.

[20] Briuglia ML, et al. Influence of cholesterol on liposome stability and on in vitro drug release. Drug Del Translational Researc. 2015;5(3):231–242.

[21] Jangra S, et al. In-vitro drug release kinetics studies of mesoporous SBA-15-azathioprine composite. J Porous Mater. 2016;23(3):679–688.

[22] Matshetshe KI, et al. Preparation, characterization and in vitro release study of β-cyclodextrin/chitosan nanoparticles loaded Cinnamomumzeylanicum essential oil. Int J Biol Macromol. 2018;118:676–682.

[23] Elzoghby AO, et al. Swellable floating tablet based on spray-dried casein nanoparticles: near-infrared spectral characterization and floating matrix evaluation. Int J Pharm (Amst). 2015;491(1–2):113–122.

[24] Bodoira RM, et al. Chia (Salvia hispanica L.) oil stability: study of the effect of natural antioxidants. LWT. 2017;75:107–113.

[25] Kozlowska J, Stachowiak N, Pru W. Stability studies of collagen-based microspheres with Calendula officinalis flower extract. Polym Degrad Stabil. 2019;163:214–219.

[26] Mazumder R, Allamneni Y, Firdous SM, Parya H, Chowdhury AD. Formulation, development and in-vitro release effects of ethyl cellulose coated pectin microspheres for colon targeting. Asian J Pharmaceut Clin Res. 2013;6(5):138–144.

[27] Zhuang J, Li M, Pu Y, Ragauskas AJ, Yoo CG. Observation of potential contaminants in processed biomass using fourier transform infrared spectroscopy. Appl Sci. 2020;10:4345.

[28] Gill P, Moghadam TT, Ranjbar B. Differential scanning calorimetry techniques: applications in biology and nanoscience. Journal of Bimolecular Techniques. 2010;21(4):167–193.

[29] Hung SF, Hsieh CM, Chen YC, Lin CM, Ho HO, Sheu MT. Formulation and process optimization of multiparticulate pulsatile system delivered by osmotic pressure-activated rupturable membrane. Int J Pharm (Amst). 2015;480(1–2):15–26.

[30] Shah RB, Tawakkul MA, Khan MA. Comparative evaluation of flow for pharmaceutical powders and granules. AAPS PharmSciTech. 2008;9(1):250–258.

[31] Mazumder R, Mahanti B, Majumdar S, Pal R, Chowdhury AD. Response surface method for optimization of prepared satranidazole powder layered pellets. Future J Pharmaceut Sci. 2021;7:190.

[32] Patel KS, Patel MB. Preparation and evaluation of chitosan microspheres containing nicorandil. Int J Pharm Investig. 2014;4(1):32–37.

[33] Swain S, Behera A, Dinda SC, et al. Formulation design, optimization and pharmacodynamic evaluation of sustained release mucoadhesive microcapsules of venlafaxine HCl. Indian J Pharmaceut Sci. 2014;76(4):354–363.

[34] Iyer V, et al. Impact of formulation and particle size on stability and immunogenicity of oil-in-water emulsion adjuvants. Hum Vaccines Immunother. 2015;11(7):1853–1864.

RIGHTS & PERMISSIONS

2024 2024 The Authors. Publishing services by Elsevier B.V. on behalf of KeAi Communications Co. Ltd.