Gastroretentive drug delivery system of levofloxacin hemihydrate: Development and evaluation of mucoadhesive microspheres for the treatment of H. pylori infection

Manodhini S. Elakkiya; Sambath R. Kumar; N. Venkateswaramurthy; D. Kamalakannan

doi:10.53730/ijhs.v6nS10.13326

Authors

Manodhini Elakkiya S. Department of Pharmaceutics, J. K. K. Nattraja College of Pharmacy, Komarapalayam, Namakkal, India-638483, Affiliated by The Tamilnadu Dr. M.G.R Medical University, Chennai
Sambath Kumar R.
sambathkumar.r@jkkn.ac.in
Department of Pharmaceutics, J. K. K. Nattraja College of Pharmacy, Komarapalayam, Namakkal, India-638483, Affiliated by The Tamilnadu Dr. M.G.R Medical University, Chennai
Venkateswaramurthy N. Department of Pharmaceutics, J. K. K. Nattraja College of Pharmacy, Komarapalayam, Namakkal, India-638483, Affiliated by The Tamilnadu Dr. M.G.R Medical University, Chennai
Kamalakannan D. Department of Pharmaceutics, J. K. K. Nattraja College of Pharmacy, Komarapalayam, Namakkal, India-638483, Affiliated by The Tamilnadu Dr. M.G.R Medical University, Chennai

Keywords:

mucoadhesive polymers, levofloxacin, microcapsules, In-vitro drug release

Abstract

The aim of the studies to formulate and develop mucoadhesive microcapsules of levofloxacin hemihydrates by using the mucoadhesive polymers for the treatment of H. pylori infection. Methods: Microspheres were prepared by Ionotropic gelation technique. To achieve the mucoadhesive and extended release property in this study, sodium alginate, chitosan and calcium chloride for formulating levofloxacin hemihydrate microcapsules. In vitro drug release and in-vitro mucoadhesiveness. Results: To achieve the mucoadhesive and extended release property in this study, mucoadhesive polymer, such as chitosan was used. Sodium dioctyl sulphosuccinate (DOSS) used as surfactant. The percentage yield for levofloxacin hemihydrate loaded microspheres was found to be in the range of 32.11±1.25% to 87.28±1.67%. Drug content of the levofloxacin hemihydrate loaded microspheres varied from 20.21±1.01% to 30.77±1.88%. The encapsulation efficiency of the prepared microspheres varied from 51.77±1.33% to 78.54±1.55%. The mean diameter of levofloxacin hemihydrate loaded microspheres were found to be in the range of 135.5±3.64 μm to 448.59±5.44μm Mucoadhesive property of the prepared microspheres varied from 45.81±1.32% to 82.97±0.82%. A signiﬁcant decrease in the rate and extent of drug release was observed with the increase in sodium alginate concentration in beads.

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References

Ansari S, Yamaoka Y: Survival of Helicobacter pylori in gastric acidic territory. Helicobacter. 2017; 22(4):e12386.

Bogataj M, Mrhar A, Grabnar I, Rajtman Z, Bukovec P, Srcic S, Urleb U. The influence of magnesium stearate on the characteristics of mucoadhesive microspheres. J Micro encapsul. 2000; 17(4):499-508.

Chun MK, Sah H, Choi HK. Preparation of mucoadhesive microspheres containing antimicrobial agents for eradication of H. pylori. Int J Pharm. 2005; 297(1-2): 172-179

Das MK, Senapati PC. Evaluation of furosemide-loaded alginate microspheres prepared by ionotropic external gelation technique. Acta Poloniae Pharmaceutica- Drug Research. 2007; 64(6):253-26.

Dhawan S1, Singla AK, Sinha VR. Evaluation of mucoadhesive properties of chitosan microspheres prepared by different methods. AAPS Pharm Sci Tech. 2004; 5(4):60-67.

Hooi JKY, Lai WY, Ng WK, et al. : Global Prevalence of Helicobacter pylori Infection: Systematic Review and Meta-Analysis. Gastroenterology. 2017; 153 (2):420–9.

Jain SK, Jangdey MS. Lectin conjugated gastro retentive multi particulate delivery system of clarithromycin for the effective treatment of Helicobacter pylori. Mol Pharm. 2009; 6(1): 295-304

Jiang J, Chen Y, Shi J, et al.: Population attributable burden of Helicobacter pylori-related gastric cancer, coronary heart disease, and ischemic stroke in China. Eur J ClinMicrobiol Infect Dis. 2017; 36(2):199–212.

Maleque, M., Hasan, M. R., Hossen, F., & Safi, S. (2012). Development and validation of a simple UV spectrophotometric method for the determination of levofloxacin both in bulk and marketed dosage formulations. Journal of Pharmaceutical Analysis, 2(6), 454–457.

Nagda CD, Chotai NP, Patel SB, Soni TJ, Patel ULN. Preparation

and in vitro evaluation of bioadhesive micro particulate systems. Int J Pharm

Sci Nano technol. 2008;1(6):266-75.

Narkar M, Sher P, Pawar A. Stomach-specific controlled release gellan beads of acid-soluble drug prepared by ionotropic gelation method. AAPS Pharm Sci Tech. 2010; 11(1): 267-277.

Obeidat, W. M., & Price, J. C. (2003). Viscosity of polymer solution phase and other factors controlling the dissolution of theophylline microspheres prepared by the emulsion solvent evaporation method. Journal of Microencapsulation, 20(1), 57–65.

Pandey, P., Saini, M., & Neeta. (2017). Mucoadhesive drug delivery system: an overview. Pharmaceutical and Biological Evaluations, 4(4), 183.

Patel JK, Chavda JR. Formulation and evaluation of stomach-specific amoxicillin-loaded carbopol-934P mucoadhesive microspheres for Anti-Helicobacter pylori therapy. J Micro encapsul. 2009; 26(4): 365-376.

Rajinikanth P.S, Sankar C, Mishra, B. Sodium alginate microsphere of metoprolol tartarate for intranasal systemic delivery: development and evaluation. Drug Deliv.2003; 10(4):21-28.

Rao MR, Borate SG, Thanki KC, Ranpise AA, Parikh GN. Development and in vitro evaluation of floating rosiglitazone maleate beads. Drug Dev Ind Pharm. 2009; 35(7):834-842.

Rao MR, Borate SG, Thanki KC, Ranpise AA, Parikh GN. Development and in vitro evaluation of floating rosiglitazone maleate microspheres. Drug Dev Ind Pharm. 2009;35(7):834-842.

Shadab, Ahuja A, Khar RK, Baboota S, Chuttani K, Mishra AK, Ali J. Gastro retentive drug delivery system of acyclovir-loaded alginate mucoadhesive microspheres: formulation and evaluation. Drug Deliv. 2011;18(4):255-264.

V. V. Khutoryanskiy. (2011). Advances in mucoadhesion and mucoadhesive polymers. Macromol Biosci, 11(6), 748-764

Zamani M, Ebrahimtabar F, Zamani V, et al.: Systematic review with meta-analysis: the worldwide prevalence of Helicobacter pylori infection. Aliment Pharma col Ther. 2018; 47(7):868–76.