Formulation of sildenafil citrate loaded nasal microsphers: An in vitro, ex vivo characterization
Keywords:
Gellan gum, Microsperes, Spray drying, Sildinafil citrate, Nasal deliveryAbstract
The aim of the present study was to prepare gellan gum microspheres of Sildenafil citrate, for intranasal delivery to avoid the first pass metabolism. The microspheres were prepared using spray drying method. The microspheres were evaluated for characteristics like particle size, incorporation efficiency, swelling ability, zeta potential, in-vitro mucoadhesion, ex-vivo mucoadhesion, thermal analysis, XRD study and invitro drug release. Treatment of in-vitro data to different kinetic equations indicated diffusion controlled drug delivery from gellan gum microspheres. The results of DSC and XRD studies revealed the molecular amorphous dispersion of Sildenafil citrate into the gellan gum microspheres. Microspheres so prepared were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 95-98%. The formulation exhibited a good mucoadhesive strength which was determined in in vitro conditions through falling film technique and was compared with ex vivo studies. The microspheres so prepared also exhibited a good swelling index which confirmed the strong mucoadhesive property of the formulation.
References
Agnihotri SA, Jawalkar SS, Aminbhavi TM.
Controlled release of cephalexin through gellan
gum beads: Effect of formulation parameters on
entrapment efficiency, size and drug release, Eur. J
of Pharm and Biopharm, 2006; 63:249-261.
Kang KS, Veeder GT, Mirrasoul PJ, Cottrel IW.
Agar like polysaccharide produced by
Pseudomonas species: production and basic
properties, Appl.Environ.Microbiol, 1982;
:1086-1091
Jansson PE, Lindberg B, Sanford PA. Structural
studies of gellan gum an extra cellular
polysaccharide elaborated by Pseudomonas eloda,
Carbohydr.Res 1983;124:135-139.
Rozier A, Mazuel C, Grove J. Functionality testing
of gellan gum, a polymeric exciepient material for
ophthalmic dosage forms, Int. J
Pharm.1997;153:191-198.
Miyazaki S, Kawasaki N, Kubo W, Endo K,
Attwood D. Comparison of insitu gellig
formulations for the oral delivery of cimetidine, Int.
J Pharm.2001; 200:161-168.
Kubik H, Muller BW. Rheological properties of
polymer solutions as carrier for nasal drug delivery
systems. Eur .J. Pharm and Biopharm, 1993;
:192-196.
Jasson B, Hagerstrom H, Fransen N. The influence
of gellan gum on the transfer of flurecein dextran
across rat nasal epithelium in vivo,
Eur.J.Pharm.Biopharm, 2005;59:557-564.
Fu-De C, Ming-Shi Y, Ben-Gang Y. Yu-Ling F,
Liang W, Peng Y, He Y.preparation of sustainedrelease nitrendipine microspheres with eudragit RS
and aerosol using quasi-emulsion solvent diffusion
method. Int. J. Pharm, 2003; 259:103-113.
Cerchiara T, Luppi B, Chidichimo G, Bigicci M,
zecchi V. Chitosan and poly(methyl vinyl ether-comaleic anhydride) microparticles as nasal sustained
delivery systems, Eur. J. Pharm and Biopharm,
;61:195-200.
Juan JT, Alfredo GA, Santiago TS, Luis G. Spraydried powders as nasal absorption enhancers of
cynocobalamine. Bio Pharm Bull, 2001; 24:1411-
Rita JM, Pradip KG, Manish LU, Rayasa SR.
Thermoreversible mucoadhesive gel for nasal
delivery of sumatryptan, AAPS PharmSciTech,
;7:E1-E7.
Tin. TY, Gonda I, Gipps EM, Miicrospheres of
polyvinyl alcohol for nasal delivery-I generation by
spray drying and spray desolvation. Pharm Res,
; 9:1330-1335.
Sarapan H, Vimolmas L, Narueporn S, Garnpimol
CR. Sparay dried mucoadhesive microspheres:
preparation and transport through nasal cell
monolayer. AAPS PharmSciTech, 2006; 7: E1-E10.
Pavenetto F, Conti B, Genta I. Solvent evaporation,
solvent extraction and spray drying for polylactide
microspheres preparation. Int. J. Pharm. Sci, 1992;
:151:159.
Illum L, Jorgensen H, Bisgard H, Rossing N.
Bioadhesive microspheres as a potential nasal drug
delivery system. Int. J. Pharm. Sci., 1987; 39:189-
Smart JD. The basic and underlying mechanisms of
mucoadhesion, Adv. Drug. Del.Rev, 2005;
:1556-1568.
Highuchi T. Mechanism of sustained action
medication. J Pharm.Sci, 1963; 52:1145-1149.
Peppas NA. Analysis of fickian and non fickian
drug release from polymers. Pharmaceutica Acta
Helvetiae, 1985; 60:110-111.
Ritger PL, Peppas NA. Simple equation for
description of solute swellable devices,
J.Control.Rel. 1987; 5:37-42.
