The present study is aimed at formulation of alginate (ALG) microspheres with ranitidine (RNT) by the spray drying method. Obtained microspheres were characterized for particle size, surface morphology, entrapment efficiency, drug loading, in vitro drug release and zeta potential. Mucoadhesive properties were examined by a texture analyser and three types of adhesive layers - gelatine discs, mucin gel and porcine stomach mucosa. Microspheres showed a smooth surface with narrow particle size distribution and RNT loading of up to 70.9 %. All formulations possessed mucoadhesive properties and exhibited prolonged drug release according to the first-order kinetics. DSC reports showed that there was no interaction between RNT and ALG. Designed microspheres can be considered potential carriers of ranitidine with prolonged residence time in the stomach
If the inline PDF is not rendering correctly, you can download the PDF file here.
1. A. R. Kumar and P. O. Katz Functional esophageal disorders: a review of diagnosis and management Expert Rev. Gastroenterol. Hepatol. 7 (2013) 453-461; DOI: 10.1586/17474124.2013.811028.
2. A. W. Basit and L. F. Lacey Colonic metabolism of ranitidine: implications for its delivery and absorption Int. J. Pharm. 227 (2001) 157-165; DOI: 10.1016/S0378-5173(01)00794-3.
3. M. F. Williams G. E. Dukes W. Heizer Y. H. Han D. J. Hermann T. Lampkin and L. J. Hak Influence of gastrointestinal site of drug delivery on the absorption characteristics of ranitidine Pharm. Res. 9 (1992) 1190-1194.
4. A. D. Khan and M. Bajpai Floating drug delivery system: an overview Int. J. PharmTech Res. 2 (2010) 2497-2505.
5. A. Streubel J. Siepmann and R. Bodmeier Gastroretentive drug delivery systems Expert Opin. Drug Deliv. 2 (2006) 217-233; DOI: 10.1517/17425247.3.2.217.
6. M. D. Shadab G. K. Singh A. Ahuja R. K. Khar S. Babota J. K. Sahni and J. Ali Mucoadhesive microspheres as a controlled drug delivery system for gastroretention Syst. Rev. Pharm. 3 (2012) 4-14; DOI: 10.4103/0975-8453.107130.
7. A. Kumar S. Jha R. Rawal P. S. Chauhan and S. D. Maurya Mucoadhesive microspheres for novel drug delivery system: a review Am. J. PharmTech Res. 3 (2013) 196-213.
8. M. Shadab A. Ahuja R. K. Khar S. Baboota K. Chu_ ani A. K. Mishra and J. Ali Gastroretentive drug delivery system of acyclovir-loaded alginate mucoadhesive microspheres: formulation and evaluation Drug Deliv. 18 (2011) 255-264; DOI: 10.3109/10717544.2010.536270.
9. H. H. Tonnesen and J. Karlsen Alginate in drug delivery systems Drug Dev. Ind. Pharm. 28 (2002) 621-630; DOI: 10.1081/DDC-120003853%20.
10. K. N. Sachan S. Pushkar A. Jha and A. Bha_ charya Sodium alginate: the wonder polymer for controlled drug delivery J. Pharm. Res. 2 (2009) 1191-1199.
11. A. L. Ching C. V. Liew L. W. Chan and P. W. Heng Modifying matrix micro-environmental pH to achieve sustained drug release from highly laminating alginate matrices Eur. J. Pharm. Sci. 33 (2008) 361-370; DOI: 10.1016/j.ejps.2008.01.007.
12. P. Zentilin P. Dulbecco E. Savarino A. Parodi E. Iiritano C. Bilardi S. Reglioni S. Vigneri and V. Savarino An evaluation of the antireflux properties of sodium alginate by means of combined multichannel intraluminal impedance and pH-metry Aliment. Pharmacol. Ther. 21 (2005) 29-34; DOI: 10.1111/j.1365-2036.2004.02298.x.
13. K. Cal and K. Sollohub Spray drying technique. I: Hardware and process parameters J. Pharm. Sci. 99 (2010) 575-586; DOI: 10.1002/jps.21886.
14. C. A. Lau-Cam M. Rahman and R. W. Roos Rapid reversed phase high performance liquid chromatographic assay method for ranitidine hydrochloride in dosage forms J. Liq. Chromatogr. 17 (1994) 1089-1104; DOI: 10.1080/10826079408013387.
15. B. Arica S. Calis P. Atilla N. T. Durlu N. Cakar H. S. Kas and A. A. Hincal In vitro and in vivo studies of ibuprofen-loaded biodegradable alginate beads J. Microencapsul. 22 (2005) 153-165; DOI: 10.1080/02652040400026319.
16. J. D. Clogston and A. K. Patri Zeta potential measurement Methods Mol. Biol. 697 (2011) 63-70; DOI: 10.1007/978-1-60327-198-1_6.
17. R. Shaikh T. R. Raj Singh M. J. Garland A. D. Woolfson and R. F. Donnelly Mucoadhesive drug delivery systems J. Pharm. Bioallied Sci. 3 (2011) 89-100; DOI: 10.4103/0975-7406.76478.
18. S. J. Jackson and A. C. Perkins In vitro assessment of the mucoadhesion of cholestyramine to porcine and human gastric mucosa Eur. J. Pharm. Biopharm. 52 (2001) 121-127; DOI: 10.1016/S0939-6411(01)00156-4.
19. P. Stasiak M. Placzek P. Lepek and M. Sznitowska Influence of polymer type active substance and experimental model on mucoadhesive properties of selected drug formulations J. Disp. Sci. Technol. 32 (2011) 1780-1785; DOI: 10.1080/01932691.2011.616175.
20. E. Szymańska K. Winnicka A. Amelian and U. Cwalina Vaginal chitosan tablets with clotrimazole - design and evaluation of mucoadhesive properties using porcine vaginal mucosa mucin and gelatin Chem. Pharm. Bull. 62 (2014) 160-167; DOI: 10.1248/cpb.c13-00689.
21. E. I. Nep and B. R. Conway Grewia gum 2: mucoadhesive properties of compacts and gels Trop. J. Pharm. Res. 10 (2011) 393-401; DOI: 10.4314/tjpr.v10i4.4.
22. The United States Pharmacopeia 35 National Formulatory 27 Vol. 1 The United States Pharmacopeial Convention Rockville 2012 pp. 264-271.
23. E. Szymańska and K. Winnicka Preparation and in vitro evaluation of chitosan microgranules with clotrimazole Acta Pol. Pharm. 69 (2012) 509-513.
24. P. Costa and J. M. Sousa Lobo Modeling and comparison of dissolution profiles Eur. J. Pharm. Sci. 13 (2001) 123-133; DOI: 10.1016/S0928-0987(01)00095-1.
25. J. Siepmann and N. A. Peppas Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC) Adv. Drug Deliv. Rev. 48 (2001) 139-157; DOI: 10.1016/S0169-409X(01)00112-0.
26. E. Mazurek-Wądołkowska K. Winnicka A. Czajkowska-Kośnik U. Czyżewska and W. Miltyk Application of diff erential scanning calorimetry in evaluation of solid state interactions in tablets containing acetaminophen Acta Pol. Pharm. 70 (2013) 787-793.
27. P. Upadhyay K. S. Khomane L. Kumar and K. A. Bansal Relationship between crystal structure and mechanical properties of ranitidine hydrochloride polymorphs Cryst. Eng. Commun. 15 (2013) 3959-3964; DOI: 10.1039/C3CE40201K.
28. N. Chieng Z. Zujovic G. Bowmaker T. Rades and D. Saville Eff ect of milling conditions on the solid-state conversion of ranitidine hydrochloride form 1 Int. J. Pharm. 327 (2006) 36-44; DOI: 10.1016/j.ĳ pharm.2006.07.032.
29. N. R. Pani L. K. Nath and S. Acharya Compatibility studies of nateglinide with excipients in immediate release tablets Acta Pharm. 61 (2011) 237-247; DOI: 10.2478/v10007-011-0016-4.
30. J. P. Soares J. E. Santos G. O. Chierice and E. T. G. Cavalheiro Thermal behavior of alginic acid and its sodium salt Ecletica Quimica 29 (2004) 57-64; DOI: 10.1590/S0100-46702004000200009.