Benzocaine loaded solid lipid nanoparticles: Formulation design, in vitro and in vivo evaluation of local anesthetic effect

Current Drug Delivery

Volumn 12, Issue 6, 2015, Pages 680-692

  Basha, Mona ^a   El Alim, Sameh Hosam Abd ^a   Kassem, Ahmed Alaa ^a   Awdan, Sally El ^a   Awad, Gamal ^a  

^a NATIONAL RESEARCH CENTRE   (Egypt)

Author keywords

Benzocaine; Design of experiment; Local anesthetic; Polyoxyethylene sorbitan fatty acid esters; Solid lipid nanoparticles; Topical anesthesia

Indexed keywords

BENZOCAINE; FATTY ACID; POLYSORBATE; POLYSORBATE 20; POLYSORBATE 40; POLYSORBATE 60; POLYSORBATE 80; SOLID LIPID NANOPARTICLE; DRUG CARRIER; HYDROGEL; LIPID; LOCAL ANESTHETIC AGENT; NANOPARTICLE; SURFACTANT;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG DELIVERY SYSTEM; DRUG DESIGN; DRUG FORMULATION; FACTORIAL DESIGN; HYDROGEL; IN VITRO STUDY; IN VIVO STUDY; KINETICS; LOCAL ANESTHESIA; MALE; NONHUMAN; PARTICLE SIZE; PRIORITY JOURNAL; RAT; SURFACE PROPERTY; SUSTAINED DRUG RELEASE; X RAY POWDER DIFFRACTION; ZETA POTENTIAL; ANIMAL; CHEMISTRY; DRUG RELEASE; MEDICINAL CHEMISTRY; PROCEDURES; TOPICAL DRUG ADMINISTRATION; WISTAR RAT; X RAY DIFFRACTION;

ADMINISTRATION, TOPICAL; ANESTHETICS, LOCAL; ANIMALS; BENZOCAINE; CALORIMETRY, DIFFERENTIAL SCANNING; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; DRUG COMPOUNDING; DRUG DELIVERY SYSTEMS; DRUG DESIGN; DRUG LIBERATION; HYDROGELS; LIPIDS; MALE; NANOPARTICLES; PARTICLE SIZE; RATS; RATS, WISTAR; SURFACE-ACTIVE AGENTS; X-RAY DIFFRACTION;

EID: 84953397172     PISSN: 15672018     EISSN: 18755704     Source Type: Journal    
DOI: 10.2174/1567201812666150703115126     Document Type: Article

References (68)

1. Barratt, G.M. Therapeutic applications of colloidal drug carriers. Pharm. Sci. Technol. Today, 2000, 3(5), 163-171.
2. Barratt, G. Colloidal drug carriers: achievements and perspectives. Cell Mol. Life Sci., 2003, 60(1), 21-37.
3. Basha, M.; Abd El-Alim, S.H.; Shamma, R.N.; Awad, G.E. Design and optimization of surfactant-based nanovesicles for ocular delivery of Clotrimazole. J. Liposome Res,. 2013, 23(3), 203-10.
4. Mozafari, M.R. Nanocarrier Technologies: Frontiers of Nanotherapy. 1st ed. 2006, Dordrecht: Springer.
5. Almeida, A.J.; Souto, E. Solid lipid nanoparticles as a drug delivery system for peptides and proteins. Adv. Drug Deliv Rev., 2007, 59(6), 478-90.
6. Suresh, G.; Manjunath, K.; Venkateswarlu, V.; Satyanarayana, V. Preparation, characterization, and in vitro and in vivo evaluation of lovastatin solid lipid nanoparticles. AAPS PharmSciTech., 2007, 8(1), 24.
7. Khalil, R.M.; Abd-Elbary, A.; Kassem, M.A.; Ghorab, M.M.; Basha, M. Nanostructured lipid carriers (NLCs) versus solid lipid nanoparticles (SLNs) for topical delivery of meloxicam. Pharm. Dev. Technol., 2014, 19(3), 304-14.
8. Muller, R.H.; Ruhl, D.; Runge, S.; Schulze-Forster, K.; Mehnert, W. Cytotoxicity of solid lipid nanoparticles as a function of the lipid matrix and the surfactant. Pharm. Res., 1997, 14(4), 458-62.
9. Heydenreich, A.V.; Westmeier, R.; Pedersen, N.; Poulsen, H.S.; Kristensen, H.G. Preparation and purification of cationic solid lipid nanospheres--effects on particle size, physical stability and cell toxicity. Int. J. Pharm., 2003, 254(1), 83-7.
10. Schwarz, C.; Mehnert, W. Solid lipid nanoparticles (SLN) for controlled drug delivery. II. Drug incorporation and physicochemical characterization. J. Microencapsul., 1999, 16(2), 205-13.
11. Rowe, R.C.; Sheskey, P.J.; Quinn, M.E. Handbook of Pharmaceutical Excipients. 6th ed. 2009, London; Chicago: Pharmaceutical Press & American Pharmacists Association.
12. Martin, M.D.; Ramsay, D.S.; Whitney, C.; Fiset, L.; Weinstein, P. Topical anesthesia: differentiating the pharmacological and psychological contributions to efficacy. Anesth. Prog., 1994, 41(2), 40-7.
13. Musawi, A.A.; Andersson, L. Use of topical as only anesthetic for suturing a traumatic facial laceration. Dent. Traumatol., 2010, 26(3), 292-3.
14. Friedman, P.M.; Fogelman, J.P.; Nouri, K.; Levine, V.J.; Ashinoff, R. Comparative study of the efficacy of four topical anesthetics. Dermatol. Surg., 1999, 25(12), 950-4.
15. Friedman, P.M.; Mafong, E.A.; Friedman, E.S.; Geronemus, R.G. Topical anesthetics update: EMLA and beyond. Dermatol. Surg., 2001, 27(12), 1019-26.
16. de Araujo, D.R.; Padula, C.; Cereda, C.M.; Tofoli, G.R.; Brito, R.B., Jr.; de Paula, E.; Nicoli, S.; Santi, P. Bioadhesive films containing benzocaine: correlation between in vitro permeation and in vivo local anesthetic effect. Pharm. Res., 2010, 27(8), 1677-86.
17. de Araujo, D.R.; da Silva, D.C.; Barbosa, R.M.; Franz-Montan, M.; Cereda, C.M.; Padula, C.; Santi, P.; de Paula, E. Strategies for delivering local anesthetics to the skin: focus on liposomes, solid lipid nanoparticles, hydrogels and patches. Expert Opin. Drug Deliv., 2013, 10(11), 1551-63.
18. Roos, T.C.; Merk, H.F. Allergic contact dermatitis from benzocaine ointment during treatment of herpes zoster. Contact Dermatitis, 2001, 44(2), 104.
19. de Padua, C.A.; Schnuch, A.; Nink, K.; Pfahlberg, A.; Uter, W. Allergic contact dermatitis to topical drugs--epidemiological risk assessment. Pharmacoepidemiol. Drug Saf., 2008, 17(8), 813-21.
20. Young, K.D. What's new in topical anesthesia. Clin Pediatr Emerg Med, 2007, 8, 232-239.
21. de Melo, N.F.; Grillo, R.; Guilherme, V.A.; de Araujo, D.R.; de Paula, E.; Rosa, A.H.; Fraceto, L.F. Poly(lactide-co-glycolide) nanocapsules containing benzocaine: influence of the composition of the oily nucleus on physico-chemical properties and anesthetic activity. Pharm. Res., 2011, 28(8), 1984-94.
22. Pradhan, M.; Singh, D.; Singh, M.R. Development characterization and skin permeating potential of lipid based novel delivery system for topical treatment of psoriasis. Chem. Phys. Lipids, 2015, 186, 9-16.
23. Pardeike, J.; Hommoss, A.; Muller, R.H. Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. Int. J. Pharm., 2009, 366(1-2), 170-84.
24. Prow, T.W.; Grice, J.E.; Lin, L.L.; Faye, R.; Butler, M.; Becker, W.; Wurm, E.M.; Yoong, C.; Robertson, T.A.; Soyer, H.P.; Roberts, M.S. Nanoparticles and microparticles for skin drug delivery. Adv. Drug Deliv. Rev., 2011, 63(6), 470-91.
25. Schafer-Korting, M.; Mehnert, W.; Korting, H.C. Lipid nanoparticles for improved topical application of drugs for skin diseases. Adv. Drug Deliv. Rev., 2007, 59(6), 427-43.
26. Manjunath, K.; Venkateswarlu, V. Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration. J. Control Release, 2005, 107(2), 215-28.
27. Venkateswarlu, V.; Manjunath, K. Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles. J Control Release, 2004, 95(3), 627-38.
28. Grillo, R.; de Melo, N.F.; de Araujo, D.R.; de Paula, E.; Dias Filho, N.L.; Rosa, A.H.; Fraceto, L.F. Validation of an HPLC Method for quantitative Determination of Benzocaine in PHBV-Microparticles and PLA-Nanoparticles. Latin Am. J. Pharm., 2009, 28(3), 393-399.
29. D'Amour, F.E.; Smith, D.L. A method for determining loss of pain sensation. J. Pharmacol. Exp. Ther., 1941, 72(1), 74-78.
30. Lukowski, G.; Kasbohm, J.; Pflegel, P.; Illing, A.; Wulff, H. Crystallographic investigation of cetylpalmitate solid lipid nanoparticles. Int. J. Pharm., 2000, 196(2), 201-5.
31. Yang, R.; Gao, R.; Li, F.; He, H.; Tang, X. The influence of lipid characteristics on the formation, in vitro release, and in vivo absorption of protein-loaded SLN prepared by the double emulsion process. Drug Dev. Ind. Pharm., 2011, 37(2), 139-48.
32. Bunjes, H.; Koch, M.H.; Westesen, K. Influence of emulsifiers on the crystallization of solid lipid nanoparticles. J.Pharm. Sci., 2003, 92(7), 1509-20.
33. Westesen, K.; Siekmann, B.; Koch, M.H.J. Investigations on the physical state of lipid nanoparticles by synchrotron radiation X-ray diffraction. Intl. J. Pharm., 1993, 93(1-3), 189-199.
34. Verbrugghe, M.; Cocquyt, E.; Saveyn, P.; Sabatino, P.; Sinnaeve, D.; Martins, J.C.; Van der Meeren, P. Quantification of hydrophilic ethoxylates in polysorbate surfactants using diffusion H1 NMR spectroscopy. J. Pharm. Biomed. Anal., 2010, 51(3), 583-9.
35. Bergh, M. Allergenic oxidation products in ethoxylated non-ionic surfactants. Chemical characterization and studies on allergenic activity and physicochemical behavior. Acta Derm. Venereol. Suppl (Stockh), 1999, 205, 1-26.
36. Lv, G.; Wang, F.; Cai, W.; Zhang, X. Characterization of the addition of lipophilic Span 80 to the hydrophilic Tween 80-stabilized emulsions. Colloids Surf. A: Physicochem. Eng. Aspects, 2014, 447, 8-13.
37. Salazar, J.; Heinzerling, O.; Muller, R.H.; Moschwitzer, J.P. Process optimization of a novel production method for nanosuspensions using design of experiments (DoE). Int. J. Pharm., 2011, 420(2), 395-403.
38. Pawar, Y.B.; Purohit, H.; Valicherla, G.R.; Munjal, B.; Lale, S.V.; Patel, S.B.; Bansal, A.K. Novel lipid based oral formulation of curcumin: development and optimization by design of experiments approach. Int. J. Pharm., 2012, 436(1-2), 617-23.
39. Ghadiri, M.; Fatemi, S.; Vatanara, A.; Doroud, D.; Najafabadi, A.R.; Darabi, M.; Rahimi, A.A. Loading hydrophilic drug in solid lipid media as nanoparticles: statistical modeling of entrapment efficiency and particle size. Int. J. Pharm., 2012, 424(1-2), 128-37.
40. Ruckmani, K.; Sankar, V. Formulation and optimization of Zidovudine niosomes. AAPS PharmSciTech., 2010, 11(3), 1119-27.
41. Devaraj, G.N.; Parakh, S.R.; Devraj, R.; Apte, S.S.; Rao, B.R.; Rambhau, D. Release studies on niosomes containing fatty alcohols as bilayer stabilizers instead of cholesterol. J. Colloid Interface Sci., 2002, 251(2), 360-5.
42. Hu, L.; Tang, X.; Cui, F. Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs. J. Pharm. Pharmacol., 2004, 56(12), 1527-35.
43. Liu, J.; Hu, W.; Chen, H.; Ni, Q.; Xu, H.; Yang, X. Isotretinoinloaded solid lipid nanoparticles with skin targeting for topical delivery. Int. J. Pharm., 2007, 328(2), 191-5.
44. Vijayan, V.; Aafreen, S.; Sakthivel, S.; Ravindra Reddy, K. Formulation and characterization of solid lipid nanoparticles loaded Neem oil for topical treatment of acne. JAD, 2013, 282-286.
45. Hao, J.; Fang, X.; Zhou, Y.; Wang, J.; Guo, F.; Li, F.; Peng, X. Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design. Int. J. Nanomed., 2011, 6, 683-92.
46. Han, F.; Li, S.; Yin, R.; Liu, H.; Xu, L. Effect of surfactants on the formation and characterization of a new type of colloidal drug delivery system: nanostructured lipid carriers. Colloids Surf A: Physicochem. Eng. Aspects, 2008, 315, 210-216.
47. Helgason, T.; Awad, T.S.; Kristbergsson, K.; McClements, D.J.; Weiss, J. Effect of surfactant surface coverage on formation of solid lipid nanoparticles (SLN). J. Colloid Interface Sci., 2009, 334(1), 75-81.
48. Gonzalez-Mira, E.; Egea, M.A.; Garcia, M.L.; Souto, E.B. Design and ocular tolerance of flurbiprofen loaded ultrasound-engineered NLC. Colloids Surf B Biointerfaces, 2010, 81(2), 412-21.
49. Aditya, N.P.; Shim, M.; Lee, I.; Lee, Y.; Im, M.H.; Ko, S. Curcumin and genistein coloaded nanostructured lipid carriers: in vitro digestion and antiprostate cancer activity. J. Agric Food Chem., 2013, 61(8), 1878-83.
50. Choi, K.O.; Aditya, N.P.; Ko, S. Effect of aqueous pH and electrolyte concentration on structure, stability and flow behavior of non-ionic surfactant based solid lipid nanoparticles. Food Chem., 2014, 147, 239-44.
51. Helgason, T.; Awad, T.S.; Kristbergsson, K.; McClements, D.J.; Weiss.J. Influence of Polymorphic Transformations on Gelation of Tripalmitin Solid Lipid Nanoparticle Suspensions. J. Am. Oil Chem. Soc., 2008, 85, 501-511.
52. Basalious, E.B.; Shawky, N.; Badr-Eldin, S.M. SNEDDS containing bioenhancers for improvement of dissolution and oral absorption of lacidipine. I: development and optimization. Int. J. Pharm., 2010, 391(1-2), 203-11.
53. Fulias, A.; Ledeti, I.; Vlase, G.; Popoiu, C.; Heghes, A.; Bilanin, M.; Vlase, T.; Gheorgheosu, D.; Craina, M.; Ardelean, S.; Ferechide, D.; Marginean, O.; Mos, L. Thermal behaviour of procaine and benzocaine Part II: compatibility study with some pharmaceutical excipients used in solid dosage forms. Chem. Cent. J., 2013, 7(1), 140.
54. Pinto, L.M.; Fraceto, L.F.; Santana, M.H.; Pertinhez, T.A.; Junior, S.O.; de Paula, E. Physico-chemical characterization of benzocaine-beta-cyclodextrin inclusion complexes. J. Pharm. Biomed. Anal., 2005, 39(5), 956-63.
55. Junyaprasert, V.B.; Teeranachaideekul, V.; Souto, E.B.; Boonme, P.; Muller, R.H. Q10-loaded NLC versus nanoemulsions: stability, rheology and in vitro skin permeation. Int. J. Pharm., 2009, 377(1-2), 207-14.
56. Sanna, V.; Caria, G.; Mariani, A. Effect of lipid nanoparticles containing fatty alcohols having different chain length on the ex vivo skin permeability of Econazole nitrate. Powder Tech., 2010, 201, 32-36.
57. Lee, C.H.; Moturi, V.; Lee, Y. Thixotropic property in pharmaceutical formulations. J.Control Release, 2009, 136(2), 88-98.
58. Han, F.; Yin, R.; Che, X.; Yuan, J.; Cui, Y.; Yin, H.; Li, S. Nanostructured lipid carriers (NLC) based topical gel of flurbiprofen: design, characterization and in vivo evaluation. Int. J. Pharm., 2012, 439(1-2), 349-57.
59. Zur, M., A.; Mehnert, W. Drug release and release mechanism of prednisolone loaded solid lipid nanoparticles. Pharmazie, 1998, 53, 552-5.
60. Pople, P.V.; Singh, K.K. Development and evaluation of topical formulation containing solid lipid nanoparticles of vitamin A. AAPS PharmSciTech., 2006, 7(4), 91.
61. Joshi, M.; Patravale, V. Formulation and evaluation of Nanostructured Lipid Carrier (NLC)-based gel of Valdecoxib. Drug Dev. Ind. Pharm., 2006, 32(8), 911-8.
62. Joshi, M.; Patravale, V. Nanostructured lipid carrier (NLC) based gel of celecoxib. Int J Pharm, 2008, 346(1-2), 124-32.
63. Mura, P.; Maestrelli, F.; Gonzalez-Rodriguez, M.L.; Michelacci, I.; Ghelardini, C.; Rabasco, A.M. Development, characterization and in vivo evaluation of benzocaine-loaded liposomes. Eur. J. Pharm. Biopharm., 2007, 67(1), 86-95.
64. Abd, El-Alim, S.H.; Kassem, A.A.; Basha, M. Proniosomes as a novel drug carrier system for buccal delivery of benzocaine. J. Drug Del. Sci. Technol., 2014, 24(5), 452-458.
65. Maestrelli, F.; Capasso, G.; Gonzalez-Rodriguez, M.L.; Rabasco, A.M.; Ghelardini, C.; Mura, P. Effect of preparation technique on the properties and in vivo efficacy of benzocaine-loaded ethosomes. J. Liposome Res., 2009, 19(4), 253-60.
66. Alvarez-Roman, R.; Naik, A.; Kalia, Y.N.; Guy, R.H.; Fessi, H. Enhancement of topical delivery from biodegradable nanoparticles. Pharm. Res., 2004, 21(10), 1818-25.
67. Cevc, G. Lipid vesicles and other colloids as drug carriers on the skin. Adv Drug Deliv Rev, 2004, 56(5), 675-711.
68. Jenning, V.; Gysler, A.; Schafer-Korting, M.; Gohla, S.H. Vitamin A loaded solid lipid nanoparticles for topical use: occlusive properties and drug targeting to the upper skin. Eur. J. Pharm. Biopharm., 2000, 49(3), 211-8.