Improved and safe transcorneal delivery of flurbiprofen by NLC and NLC-based hydrogels

Journal of Pharmaceutical Sciences

Volumn 101, Issue 2, 2012, Pages 707-725

  Gonzalez Mira, Elisabet ^a   Nikolić, Saša ^a   Calpena, Ana C ^a   Egea, M Antonia ^a   Souto, Eliana B ^b,c   García, M Luisa ^a  

^a UNIVERSITY OF BARCELONA   (Spain)

^b UNIVERSIDADE FERNANDO PESSOA   (Portugal)

^c UNIVERSITY OF TRÁS OS MONTES AND ALTO DOURO   (Portugal)

Author keywords

Drug release; Factorial design; Flurbiprofen; Hydrogels; Nanoparticles; Nanostructured lipid carriers; Ophtalmic drug delivery; Physical stability; Polymorphism; Rheology

Indexed keywords

CARBOMER; FLURBIPROFEN; NANOCARRIER; NANOSTRUCTURED LIPID CARRIER; STEARIC ACID; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CORNEA; CRYSTAL STRUCTURE; DISPERSION; DRUG ADMINISTRATION ROUTE; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG PENETRATION; EX VIVO STUDY; EXPERIMENTAL RABBIT; HYDROGEL; IN VIVO STUDY; MEAN RESIDENCE TIME; MOLECULAR STABILITY; NONHUMAN; PARTICLE SIZE; SUSTAINED DRUG RELEASE; THIXOTROPY; TRANSCORNEAL DRUG ADMINISTRATION; X RAY DIFFRACTION;

EID: 84455205699     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.22784     Document Type: Article

References (54)

1. Le Bourlais C, Acar L, Zia H, Sado PA, Needham T, Leverge R. 1998. Ophthalmic drug delivery systems-Recent advances. Prog Retin Eye Res 17:33-58.
2. Pignatello R, Bucolo C, Spedalieri G, Maltese A, Puglisi G. 2002. Flurbiprofen-loaded acrylate polymer nanosuspensions for ophthalmic application. Biomaterials 23:3247-3255.
3. Hornof M, Toropainen E, Urtti A. 2005. Cell culture models of the ocular barriers. Eur J Pharm Biopharm 60:207-225.
4. Sahoo SK, Dilnawaz F, Krishnakumar S. 2008. Nanotechnology in ocular drug delivery. Drug Discov Today 13:144-151.
5. Araújo J, Gonzalez E, Egea MA, Garcia ML, Souto EB. 2009. Nanomedicines for ocular NSAIDs: Safety on drug delivery. Nanomedicine 5:394-401.
6. Souto EB, Doktorovova S, Gonzalez-Mira E, Egea MA, Garcia ML. 2010. Feasibility of lipid nanoparticles for ocular delivery of anti-inflammatory drugs. Curr Eye Res 35:537-552.
7. Gonzalez-Mira E, Egea MA, Souto EB, Calpena AC, Garcia ML. 2011. Optimizing flurbiprofen-loaded NLC by central composite factorial design for ocular delivery. Nanotechnology 22:045101.
8. Ding S. 1998. Recent developments in ophthalmic drug delivery. Pharm Sci Technol Today 1:328-335.
9. Souto EB, Wissing SA, Barbosa CM, Müller RH. 2004. Evaluation of the physical stability of SLN and NLC before and after incorporation into hydrogel formulations. Eur J Pharm Biopharm 58:83-90.
10. Unlu N, Ludwig A, Van Ooteghem M, Hincal AA. 1992. A comparative rheological study on carbopol viscous solutions and, the evaluation of their suitability as the ophthalmic vehicles and artificial tears. Pharm Acta Helv 67:5-10.
11. Islam MT, Rodriguez-Hornedo N, Ciotti S, Ackermann C. 2004. Rheological characterization of topical carbomer gels neutralized to different pH. Pharm Res 21:1192-1199.
12. Leardi R. 2009. Experimental design in chemistry: A tutorial. Anal Chim Acta 652:161-172.
13. Araujo J, Gonzalez-Mira E, Egea MA, Garcia ML, Souto EB. 2010. Optimization and physicochemical characterization of a triamcinolone acetonide-loaded NLC for ocular antiangiogenic applications. Int J Pharm 393:167-175.
14. Westesen K, Bunjes H, Koch MHJ. 1997. Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release potential. J Control Release 48:223-236.
15. Silva AC, Santos D, Ferreira DC, Souto EB. 2009. Minoxidil-loaded nanostructured lipid carriers (NLC): Characterization and rheological behaviour of topical formulations. Pharmazie 64:177-182.
16. Reddy LH, Murthy RS. 2005. Etoposide-loaded nanoparticles made from glyceride lipids: Formulation, characterization, in vitro drug release, and stability evaluation. AAPS PharmSciTech 6:E158-E166.
17. Costa P, Sousa Lobo JM. 2001. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 13:123-133.
18. Yamaoka K, Nakagawa T, Uno T. 1978. Application of Akaike's information criterion (AIC) in the evaluation of linear pharmacokinetic equations. J Pharmacokinet Biopharm 6:165-175.
19. Valls R, Vega E, Garcia ML, Egea MA, Valls JO. 2008. Transcorneal permeation in a corneal device of non-steroidal anti-inflammatory drugs in drug delivery systems. Open Med Chem J 2:66-71.
20. Thomas ML, Szeto VR, Gan CM, Polse KA. 1997. Sequential staining: The effects of sodium fluorescein, osmolarity, and pH on human corneal epithelium. Optom Vis Sci 74:207-210.
21. Vega E, Gamisans F, Garcia ML, Chauvet A, Lacoulonche F, Egea MA. 2008. PLGA nanospheres for the ocular delivery of flurbiprofen: Drug release and interactions. J Pharm Sci 97:5306-5317.
22. Duprat P, Delsaut L, Gradiski D. 1976. Irritant power of the principle chlorinated aliphatic solvents on the skin and ocular mucosa of the rabbit. Eur J Toxicol Environ Hyg 9:171-177.
23. Kay JH, Calandra JK. 1962. Interpretation of eye irritation test. J Soc Cosmet Chem 13:281-289.
24. Passantino A. 2008. Application of the 3Rs principles for animals used for experiments at the beggining of the 21st century. Annu Rev Biomed Sci 10:27-32.
25. Shen J, Sun M, Ping Q, Ying Z, Liu W. 2010. Incorporation of liquid lipid in lipid nanoparticles for ocular drug delivery enhancement. Nanotechnology 21:025101.
26. Bogataj M, Vovk T, Kerec M, Dimnik A, Grabnar I, Mrhar A. 2003. The correlation between zeta potential and mucoadhesion strength on pig vesical mucosa. Biol. Pharm. Bull. 26:743-746.
27. Zhang J, Fan Y, Smith E. 2009. Experimental design for the optimization of lipid nanoparticles. J Pharm Sci 98:1813-1819.
28. Zhang L, Qian Y, Long C, Chen Y. 2008. Systematic procedures for formulation design of drug-loaded solid lipid microparticles: Selection of carrier material and stabilizer. Ind Eng Chem Res 47:6091-6100.
29. Li X, Nie SF, Kong J, Li N, Ju CY, Pan WS. 2008. A controlled-release ocular delivery system for ibuprofen based on nanostructured lipid carriers. Int J Pharm 363:177-182.
30. Souto EB, Mehnert W, Muller RH. 2006. Polymorphic behaviour of Compritol (R) 888 ATO as bulk lipid and as SLN and NLC. J Microencapsul 23:417-433.
31. Jenning V, Thünemann AF, Gohla SH. 2000. Characterisation of a novel solid lipid nanoparticle carrier system based on binary mixtures of liquid and solid lipids. Int J Pharm 199:167-177.
32. Precht D. 1988. Fat crystal structure in cream and butter. In Crystallization and polymorphism of fats and fatty acids; Gart N, Sato K, Eds. New York: Marcel Dekker, Inc., pp 305-355.
33. Souto EB. 2005. SLN and NLC for topical delivery of antifungals. Ph.D. Thesis. Berlin, Germany: Institute for Pharmacy, Free University of Berlin.
34. Nanjawade BK, Manvi FV, Manjappa AS. 2007. In situ-forming hydrogels for sustained ophthalmic drug delivery. J Control Release 122:119-134.
35. Buchan B, Kay G, Heneghan A, Matthews KH, Cairns D. 2010. Gel formulations for treatment of the ophthalmic complications in cystinosis. Int J Pharm 392:192-197.
36. Zignani M, Tabatabay C, Gurny R. 1995. Topical semi-solid drug delivery: Kinetics and tolerance of ophthalmic hydrogels. Adv Drug Deliv Rev 16:51-60.
37. Tamburic S, Craig DQM. 1996. The use of bioadhesive polymers as a means of improving drug delivery. In Chemical aspects of drug delivery systems; Karsa DR, Stephenson RA, Eds. 1st ed. London, UK: Royal Society of Chemistry, pp 11-40.
38. Dragicevic-Curic N, Winter S, Stupar M, Milic J, Krajisnik D, Gitter B, Fahr A. 2009. Temoporfin-loaded liposomal gels: Viscoelastic properties and in vitro skin penetration. Int J Pharm 373:77-84.
39. Hartmann V, Keipert S. 2000. Physico-chemical, in vitro and in vivo characterisation of polymers for ocular use. Pharmazie 55:440-443.
40. Schoenwald RD, Ward RL, Desantis LM, Roehrs RE. 1978. Influence of high-viscosity vehicles on miotic effect of pilocarpine. J Pharm Sci 67:1280-1283.
41. Lee CH, Moturi V, Lee Y. 2009. Thixotropic property in pharmaceutical formulations. J Control Release 136:88-98.
42. Adeyeye MC, Jain AC, Ghorab MK, Reilly WJ Jr. 2002. Viscoelastic evaluation of topical creams containing microcrystalline cellulose/sodium carboxymethyl cellulose as stabilizer. AAPS PharmSciTech 3:E8.
43. Lippacher A, Müller RH, Mäder K. 2004. Liquid and semisolid SLN™ dispersions for topical application: Rheological characterization. Eur J Pharm Biopharm 58:561-567.
44. Brummer R. 2006. Reology essentials of cosmetic and food emulsions. Berlin, Heidelberg, New York: Springer, pp 81-124.
45. Lippacher A, Muller RH, Mader K. 2002. Semisolid SLN dispersions for topical application: Influence of formulation and production parameters on viscoelastic properties. Eur J Pharm Biopharm 53:155-160.
46. Malvern Instruments. 2009. 10 ways to control rheology by changing particle properties. INFORM series of white papers.
47. Bhaskar K, Anbu J, Ravichandiran V, Venkateswarlu V, Rao YM. 2009. Lipid nanoparticles for transdermal delivery of flurbiprofen: Formulation, in vitro, ex vivo and in vivo studies. Lipids Health Dis 8:6.
48. Lippacher A, Müller RH, Mäder K. 2001. Preparation of semisolid drug carriers for topical application based on solid lipid nanoparticles. Int J Pharm 214:9-12.
49. Westesen K. 1993. Investigations on the physical state of lipid nanoparticles by synchrotron radiation X-ray diffraction. Int J Pharm 93:189.
50. Schoenwald RD, Huang HS. 1983. Corneal penetration behavior of beta-blocking agents I: Physiochemical factors. J Pharm Sci 72:1266-1272.
51. Saettone MF, Chetoni P, Cerbai R, Mazzanti G, Braghiroli L. 1996. Evaluation of ocular permeation enhancers: In vitro effects on corneal transport of four β-blockers, and in vitro/in vivo toxic activity. Int J Pharm 142:103-113.
52. Williams AC, Cornwell PA, Barry BW. 1992. On the non-Gaussian distribution of human skin permeabilities. Int J Pharm 86:69-77.
53. Attama AA, Reichl S, Muller-Goymann CC. 2009. Sustained release and permeation of timolol from surface-modified solid lipid nanoparticles through bioengineered human cornea. Curr Eye Res 34:698-705.
54. Hosny KM. 2010. Optimization of gatifloxacin liposomal hydrogel for enhanced transcorneal permeation. J Liposome Res 20:31-37.