Ropivacaine loaded microemulsion and microemulsion-based gel for transdermal delivery: Preparation, optimization, and evaluation

International Journal of Pharmaceutics

Volumn 477, Issue 1, 2014, Pages 47-56

  Zhao, Lili ^a   Wang, Yi ^b   Zhai, Yingjie ^a   Wang, Zimin ^b   Liu, Jiyong ^b   Zhai, Guangxi ^b  

^a SHANDONG UNIVERSITY   (China)

^b SECOND MILITARY MEDICAL UNIVERSITY   (China)

Author keywords

Analgesic activity; Carbopol; Microemulsion; Ropivacaine; Transdermal delivery

Indexed keywords

ACETIC ACID; ALCOHOL; CARBOMER; LABRASOL; ROPIVACAINE; WATER; AMIDE; EMULSION; EXCIPIENT; GEL; LOCAL ANESTHETIC AGENT;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG PENETRATION; DRUG SOLUBILITY; EX VIVO STUDY; GEL; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HISTOPATHOLOGY; MALE; MICROEMULSION; MOUSE; NONHUMAN; PARTICLE SIZE; PROCESS OPTIMIZATION; SKIN IRRITATION; SKIN SURFACE; TRANSDERMAL DRUG DELIVERY SYSTEM; TRANSMISSION ELECTRON MICROSCOPY; ANIMAL; CHEMISTRY; CUTANEOUS DRUG ADMINISTRATION; DISEASE MODEL; EMULSION; MEDICINAL CHEMISTRY; SKIN ABSORPTION; SOLUBILITY;

ADMINISTRATION, CUTANEOUS; AMIDES; ANESTHETICS, LOCAL; ANIMALS; CHEMISTRY, PHARMACEUTICAL; DISEASE MODELS, ANIMAL; EMULSIONS; EXCIPIENTS; GELS; MALE; MICE; MICROSCOPY, ELECTRON, TRANSMISSION; PARTICLE SIZE; SKIN ABSORPTION; SOLUBILITY;

EID: 84908221958     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2014.10.005     Document Type: Article

References (51)

1. S.M. Abdel-Hafez, R.M. Hathout, and O.A. Sammour Towards better modeling of chitosan nanoparticles production: screening different factors and comparing two experimental designs Int. Biol. Macromol. 64 2014 334 340
2. S.P. Acharya, K. Pundarikakshudu, A. Panchal, and A. Lalwani Preparation and evaluation of transnasal microemulsion of carbamazepine Asian J. Pharm. Sci. 8 2013 64 70
3. F.Q. Alvarenga, B.C. Mota, M.N. Leite, J.M. Fonseca, D.A. Oliveira, A. Royo Vde, M.L. e Silva, V. Esperandim, A. Borges, and R.S. Laurentiz In vivo analgesic activity, toxicity and phytochemical screening of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine J. Ethnopharmacol. 150 2013 280 284
4. A. Azeem, F.J. Amad, R.K. Khar, and S. Talegaonkar Nanocarrier for the transdermal delivery of an antiparkinsonian drug AAPS PharmSciTech. 10 2009 1093 1103
5. A. Azeem, S. Talegaonkar, L.M. Negi, F.J. Ahmad, R.K. Khar, and Z. Iqbal Oil based nanocarrier system for transdermal delivery of ropinirole A mechanistic pharmacokinetic and biochemical investigation Int. J. Pharm. 422 2012 436 444
6. R.M. Al Abood, S. Talegaonkar, M. Tariq, and F.J. Ahmad Microemulsion as a tool for the transdermal delivery of ondansetron for the treatment of chemotherapy induced nausea and vomiting Colloids Surf. B: Biointerfaces 101 2013 143 151
7. G. Cevc Lipid vesicles and other colloids as drug carriers on the skin Adv. Drug Deliv. Rev. 56 2004 675 711
8. A. Chatterjee, R.J. Babu, E. Ahaghotu, and M. Singh The effect of occlusive and unocclusive exposure to xylene and benzene on skin irritation and molecular responses in hairless rats Arch. Toxicol. 79 2005 294 301
9. H. Chaudhary, K. Kohli, and V. Kumar Nano-transfersomes as a novel carrier for transdermal delivery Int. J. Pharm. 454 2013 367 380
10. H. Chen, D. Mou, D. Du, X. Chang, D. Zhu, J. Liu, H. Xu, and X. Yang Hydrogel-thickened microemulsion for topical administration of drug molecule at an extremely low concentration Int. J. Pharm. 341 2007 78 84
11. B. Das, A.K. Nayak, and U. Nanda Topical gels of lidocaine HCl using cashew gum and Carbopol 940: preparation and in vitro skin permeation Int. Biol. Macromol. 62 2013 514 517
12. G.M. El Maghraby Transdermal delivery of hydrocortisone from eucalyptus oil microemulsion: effects of cosurfactants Int. J. Pharm. 355 2008 285 292
13. P.M. Elias, and G.K. Menon Structural and lipid biochemical correlates of the epidermal permeability barrier Adv. Lipid Res. 24 1991 1 26
14. J.Y. Fang, C.L. Fang, C.H. Liu, and Y.H. Su Lipid nanoparticles as vehicles for topical psoralen delivery: solid lipid nanoparticles (SLN) versus nanostructured lipid carriers (NLC) Eur. J. Pharm. Biopharm. 70 2008 633 640
15. S.A. Fouad, E.B. Basalious, M.A. El-Nabarawi, and S.A. Tayel Microemulsion and poloxamer microemulsion-based gel for sustained transdermal delivery of diclofenac epolamine using in-skin drug depot: in vitro/in vivo evaluation Int. J. Pharm. 453 2013 569 578
16. M. Goyal, M. Ghosh, B.P. Nagori, and D. Sasmal Analgesic and anti-inflammatory studies of cyclopeptide alkaloid fraction of leaves of Ziziyphus nummularia Saudi J. Biol. Sci. 20 2013 365 371
17. C. Gutton, J.P. Bellefleur, S. Puppo, J. Brunet, F. Antonini, M. Leone, and F. Bretelle Lidocaine versus ropivacaine for perineal infiltration post-episiotomy Int. J. Gynaecol. Obstet. 122 2013 33 36
18. R. Gannu, C.R. Palem, V.V. Yamsani, S.K. Yamsani, and M.R. Yamsani Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: formulation optimization, ex vivo and in vivo characterization Int. J. Pharm. 388 2010 231 241
19. R.M. Hathout, T.J. Woodman, S. Mansour, N.D. Mortada, A.S. Geneidi, and R.H. Guy Microemulsion formulations for the transdermal delivery of testosterone Eur. J. Pharm. Sci. 40 2010 188 196
20. R.M. Hathout, and A.H. Elshafeey Development and characterization of colloidal soft nano-carriers for transdermal delivery and bioavailability enhancement of an angiotensin II receptor blocker Eur. J. Pharm. Biopharm. 82 2012 230 240
21. R.M. Hathout, and M. Nasr Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization biophysical assessment, confocal imaging and permeation studies Colloids Surf. B: Biointerfaces 110 2013 254 260
22. E. Jung, Y.P. Kang, I.S. Yoon, J.S. Kim, S.W. Kwon, S.J. Chung, C.K. Shim, and D.D. Kim Effect of permeation enhancers on transdermal delivery of fluoxetine: in vitro and in vivo evaluation Int. J. Pharm. 456 2013 362 369
23. S. Kano, and K. Sugibayashi Kinetic analysis on the skin disposition of cytotoxicity as an index of skin irritation produced by cetylpyridinium chloride comparison of in vitro data using a three-dimensional cultured human skin model with in vivo results in hairless mice Pharm. Res. 23 2006 329 335
24. Y.C. Kau, K.M. Wong, M.H. Shyr, Y.H. Lee, and T.H. Tsai Simultaneous determination of unbound ropivacaine in rat blood and brain using microdialysis J. Chromatogr. B: Biomed. Sci. Appl. 760 2001 107 112
25. S. Khurana, N.K. Jain, and P.M. Bedi Nanoemulsion based gel for transdermal delivery of meloxicam: physico-chemical, mechanistic investigation Life Sci. 92 2013 383 392
26. M.H. Kim, D.H. Park, J.H. Yang, Y.B. Choy, and J.H. Choy Drug-inorganic-polymer nanohybrid for transdermal delivery Int. J. Pharm. 444 2013 120 127
27. R. Koster, M. Anderson, and E.J. de Beer Acetic acid for analgesic screening Fed. Proc. 18 1959 412 418
28. S. Jana, S. Manna, A.K. Nayak, K.K. Sen, and S.K. Basu Carbopol gel containing chitosan-egg albumin nanoparticles for transdermal aceclofenac delivery Colloids Surf. B: Biointerfaces 114 2014 36 44
29. K.E. Lee, Y.J. Choi, B.R. Oh, I.K. Chun, and H.S. Gwak Formulation and in vitro/in vivo evaluation of levodopa transdermal delivery systems Int. J. Pharm. 456 2013 432 436
30. G.S. Leisure, and C.A. DiFazio Ropivacaine: the new local anesthetic Semin. Anesth. Prioper. Med. Pain 15 1996 1 9
31. S. Liu, M.N. Jin, Y.S. Quan, F. Kamiyama, H. Katsumi, T. Sakane, and A. Yamamoto The development and characteristics of novel microneedle arrays fabricated from hyaluronic acid, and their application in the transdermal delivery of insulin J. Control. Release 161 2012 933 941
32. C. Matera, L. Flammini, M. Quadri, V. Vivo, V. Ballabeni, U. Holzgrabe, K. Mohr, M. De Amici, E. Barocelli, S. Bertoni, and C. Dallanoce Bis(ammonio) alkane-type agonists of muscarinic acetylcholine receptors: synthesis in vitro functional characterization, and in vivo evaluation of their analgesic activity Eur. J. Med. Chem. 75 2014 222 232
33. J.H. McClure Ropivacaine Brit. J. Anaesth. 76 1996 300 307
34. T. Ogiso, N. Niinaka, and M. Iwaki Mechanism for enhancement effect of lipid disperse system on percutaneous absorption J. Pharm. Sci. 85 1996 57 64
35. B.E. Polat, W.M. Deen, R. Langer, and D. Blankschtein A physical mechanism to explain the delivery of chemical penetration enhancers into skin during transdermal sonophoresis - insight into the observed synergism J. Control. Release 158 2012 250 260
36. T.W. Prow, J.E. Grice, L.L. Lin, R. Faye, M. Butler, W. Becker, E.M. Wurm, C. Yoong, T.A. Robertson, H.P. Soyer, and M.S. Roberts Nanoparticles and microparticles for skin drug delivery Adv. Drug Deliv. Rev. 63 2011 470 491
37. S.D. Roy, M. Gutierrez, G.L. Flynn, and G.W. Cleary Controlled transdermal delivery of fentanyl: characterizations of pressure-sensitive adhesives for matrix patch design J. Pharm. Sci. 85 1996 491 495
38. D.B. Scott, A. Lee, D. Fagan, G.M. Bowler, P. Bloomfield, and R. Lundh Acute toxicity of ropivacaine compared with that of bupivacaine Anesth. Analg. 69 1989 563 569
39. V. Shankarananth, N. Balakrishnan, D. Suresh, G. Sureshpandian, E. Edwin, and E. Sheeja Analgesic activity of methanol extract of Aegle marmelos leaves Fitoterapia 78 2007 258 259
40. S. Tenjarla Microemulsions: an overview and pharmaceutical applications Crit. Rev. Ther. Drug 16 1999 461 521
41. N. Ustundag Okur, S. Apaydin, N.U. Karabay Yavasoglu, A. Yavasoglu, and H.Y. Karasulu Evaluation of skin permeation and anti-inflammatory and analgesic effects of new naproxen microemulsion formulations Int. Pharm. 416 2011 136 144
42. H.K. Vaddi, P.C. Ho, and S.Y. Chan Terpenes in propylene glycol as skin-penetration enhancers: permeation and partition of haloperidol, Fourier transform infrared spectroscopy, and differential scanning calorimetry J. Pharm. Sci. 91 2002 1639 1651
43. C. Vitorino, A. Almeida, J. Sousa, I. Lamarche, P. Gobin, S. Marchand, W. Couet, J.C. Olivier, and A. Pais Passive and active strategies for transdermal delivery using co-encapsulating nanostructured lipid carriers: in vitro vs in vivo studies Eur. J. Pharm. Biopharm. 86 2014 133 144
44. C. Vitorino, J. Almeida, L.M. Goncalves, A.J. Almeida, J.J. Sousa, and A.A. Pais Co-encapsulating nanostructured lipid carriers for transdermal application: from experimental design to the molecular detail J. Control. Release 167 2013 301 314
45. Y. Yuan, S.M. Li, F.K. Mo, and D.F. Zhong Investigation of microemulsion system for transdermal delivery of meloxicam Int. J. Pharm. 321 2006 117 123
46. Y. Zhai, X. Yang, L. Zhao, Z. Wang, and G. Zhai Lipid nanocapsules for transdermal delivery of ropivacaine: in vitro and in vivo evaluation Int. J. Pharm. 471 2014 103 111
47. J. Zhang, and B. Michniak-Kohn Investigation of microemulsion microstructures and their relationship to transdermal permeation of model drugs: ketoprofen, lidocaine, and caffeine Int. J. Pharm. 421 2011 34 44
48. L. Zhao, L. Zhang, L. Meng, J. Wang, and G. Zhai Design and evaluation of a self-microemulsifying drug delivery system for apigenin Drug Dev. Ind. Pharm. 39 2013 662 669
49. X. Zhao, J.P. Liu, X. Zhang, and Y. Li Enhancement of transdermal delivery of theophylline using microemulsion vehicle Int. J. Pharm. 327 2006 58 64
50. W. Zhu, A. Yu, W. Wang, R. Dong, J. Wu, and G. Zhai Formulation design of microemulsion for dermal delivery of penciclovir Int. J. Pharm. 360 2008 184 190
51. W. Zhu, C. Guo, A. Yu, Y. Gao, F. Cao, and G. Zhai Microemulsion-based hydrogel formulation of penciclovir for topical delivery Int. J. Pharm. 378 2009 152 158