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. 2004 Sep 13;5(4):92–100. doi: 10.1208/pt050463

Effect of organogel components on in vitro nasal delivery of propranolol hydrochloride

Sambhaji Pisal 1,✉, Vjiay Shelke 1, Kakasaheb Mahadik 1, Shivajirao Kadam 1
PMCID: PMC2750488  PMID: 15760060

Abstract

The purpose of this research was to evaluate in vitro transnasal sustained-release ability of sorbitan monostearate (SMS) organogels in isopropyl myristate (IM). Organogels were prepared containing SMS (2.5%–20%) and water (5%–25%) in IM and analyzed microscopically for phase behavior. The effect of Tween surfactants on gel strength and in vitro nasal diffusion of propranolol is reported. The in vitro nasal release retardant effect of SMS and Tween 20 was investigated using factorial design. The microscopic changes in structure of organogel during in vitro nasal diffusion were studied. The water-holding capacity of SMS organogels in IM increased with SMS concentration. The release retardant effect with incorportation of cosurfactant was of the order of Tween 80> Tween 60> Tween 20. Gel strengthening and increased viscosity were evident with increased concentration of SMS and Tween 20. The 3-dimensional network of SMS molecules controls the diffusional drug release. The organogel system on nasal mucosa during diffusion is dynamic in nature and changes continuously with the time of diffusion. The water penetration in the organogel network results in percolation and emulsification of organogel, thus affecting the release. Organogels provided an effective barrier for diffusion of propranolol. The surface epithelium lining and the granular cellular structure of treated nasal mucosa were intact.

Keywords: sorbitan monostearate, organogel, nasal, propranolol, in vitro, retard release

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References

  • 1.Hussain A, Kimura R, Huang CH, Mustafa R. Nasal absorption of ergotamine tartrate in rats. Int J Pharm. 1984;21:289–293. doi: 10.1016/0378-5173(84)90187-X. [DOI] [Google Scholar]
  • 2.Pontiroli A. Intranasal calcitonin and plasma calcium concentration in normal subjects. BMJ. 1985;290:1390–1395. doi: 10.1136/bmj.290.6479.1390. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 3.Merkus FWHM, inventor. Nasal melatonin composition. US patent 6 007 834. March 26, 1998.
  • 4.Nishimoto Y, Naoki N. Powder dosage form of insulin for nasal administration. J Control Release. 1984;1:15–24. doi: 10.1016/0168-3659(84)90017-8. [DOI] [Google Scholar]
  • 5.Illum L, Critchley H, Davis SS. Nasal administration of gentamicin using novel microsphere delivery system. Int J Pharm. 1988;46:261–265. doi: 10.1016/0378-5173(88)90087-7. [DOI] [Google Scholar]
  • 6.Farraj NF, Johansen BR, Davis SS, Illum L. Nasal administration of insulin using bioadhesive microspheres as a delivery system. J Control Release. 1990;3:253–261. doi: 10.1016/0168-3659(90)90016-M. [DOI] [Google Scholar]
  • 7.Hussain AA, Foster T, Hirai S. Nasal absorption of propranolol in humans. J Pharm Sci. 1980;69:1240–1244. doi: 10.1002/jps.2600691037. [DOI] [PubMed] [Google Scholar]
  • 8.Ahn BN, Kim SK, Shim CK. Proliposomes as an intranasal dosage form for the sustained delivery of propranolol. J Control Release. 1995;4:203–210. doi: 10.1016/0168-3659(94)00114-A. [DOI] [Google Scholar]
  • 9.Vyas SP, Talwar N, Jain NK. An erythrocyte based bioadhesive system for nasal delivery of propranolol. J Control Release. 1993;23:231–237. doi: 10.1016/0168-3659(93)90004-O. [DOI] [Google Scholar]
  • 10.Tan YTF, Peh KK, Al-Hanbali O. Effect of carbopol and polyvinylpyrrolidone on the mechanical, rheological, and release properties of bioadhesive polyethylene glycol gels. AAPS PharmSciTech. 2000;1:E24–E24. doi: 10.1208/pt010324. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 11.D'Cruz OJ, Yiv SH, Uckun FM. GM-144, a novel lipophilic vaginal contraceptive gel-microemulsion. AAPS PharmSciTech. 2001;2:E5–E5. doi: 10.1208/pt020205. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 12.Pisal SS, Paradkar AR, Mahadik KR, Kadam SS. Pluronic gels for nasal delivery of vitamin B12. Part I: Preformulation study. Int J Pharm. 2004;270:37–45. doi: 10.1016/j.ijpharm.2003.10.005. [DOI] [PubMed] [Google Scholar]
  • 13.Pisal SS, Reddy P, Ketkar AR, Patil VB, Paradkar AR. Transnasal absorption of melatonin from thermo-reversible gels of pluronic PF 127 gels. Paper presented at: 62nd World Pharmaceutical Congress; September 3, 2002, Nice, France; DDT-P-039.
  • 14.Anand B, Pisal SS, Paradkar AR, Mahadik KR. Applications of organogels in pharmaceuticals. J Sci Ind Res (India). 2001;60:311–318. [Google Scholar]
  • 15.Lin Y, Kachar B, Weiss RG. Novel family of gelators of organic fluids and the structure of their gels. J Am Chem Soc. 1989;111:5542–5551. doi: 10.1021/ja00197a005. [DOI] [Google Scholar]
  • 16.Shilpa K, Rees GD, Lawrence MJ. Formation of electrically conducting microemulusion based organogels. Int J Pharm. 2003;250:65–83. doi: 10.1016/S0378-5173(02)00491-X. [DOI] [PubMed] [Google Scholar]
  • 17.Willimann H, Walde P. Lecithin organogels as matrix for transdermal transport of drugs. J Pharm Sci. 1992;81:871–874. doi: 10.1002/jps.2600810906. [DOI] [PubMed] [Google Scholar]
  • 18.Dreher F, Walde P, Walther P, Wehrli E. Interaction of lecithin microemulsion gel with human stratum corneum and its effect on transdermal transport. J Control Release. 1997;45:131–140. doi: 10.1016/S0168-3659(96)01559-3. [DOI] [Google Scholar]
  • 19.Fresta M, Puglisi G, Ventura CA, Panico AM. Lecithin organogels as potential ophthalmic drug delivery systems: a toxicology study. J Control Release. 1997;48:328–329. [Google Scholar]
  • 20.Florence AT, Murdan S, Bergh BVD, Gregoriadis G. Water-in-sorbitan monostearate organogels (water in oil gels) J Pharm Sci. 1999;88:615–619. doi: 10.1021/js980343j. [DOI] [PubMed] [Google Scholar]
  • 21.Murdan S, Gregoriadis G, Florence AT. Novel sorbitan monostearate organogels. J Pharm Sci. 1999;88:608–614. doi: 10.1021/js980342r. [DOI] [PubMed] [Google Scholar]
  • 22.Choi HG. Effect of sodium chloride on gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium. Int J Pharm. 2001;226:195–205. doi: 10.1016/S0378-5173(01)00809-2. [DOI] [PubMed] [Google Scholar]
  • 23.Pisal SS, Reddy P, Mahadik KR, Kadam SS. Nasal melatonin gels using pluronic-PF-127 for chronobiological treatment of sleep disorder.Ind J Biotech. In press.
  • 24.Goto S, Kawata M, Suzuki T, Kim NS. Preparation and evaluation of Eudragit gel. I. Eudragit organogel contining drug and rectal sustained release preparation. J Pharm Sci. 1991;80:958–961. doi: 10.1002/jps.2600801011. [DOI] [PubMed] [Google Scholar]
  • 25.Shilpa K, Rees GD, Lawrence MJ. Gelatin stabilized microemulsionbased organogels: rheology and its application in iontophoretic transdermal drug delivery. J Control Release. 1999;60:355–365. doi: 10.1016/S0168-3659(99)00092-9. [DOI] [PubMed] [Google Scholar]
  • 26.Murdan S, Gregoriadis G, Florence AT. Non-ionic surfactant organogels incorporating niosomes. STP Pharma Sci. 2004;6:44–48. [Google Scholar]
  • 27.Murdan S, Gregoriadis G, Florence AT. Interaction of nonionic surfactant based organogel with aqueous media. Int J Pharm. 1999;180:211–214. doi: 10.1016/S0378-5173(99)00007-1. [DOI] [PubMed] [Google Scholar]
  • 28.Kibbe HA. Handbook of Pharmaceutical Excipients. London, UK: American Pharmaceutical Association, Pharmaceutical Press; 2000. [Google Scholar]

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