Tags

Type your tag names separated by a space and hit enter

Natural lipids-based NLC containing lidocaine: from pre-formulation to in vivo studies.
Eur J Pharm Sci 2017; 106:102-112EJ

Abstract

In a nanotechnological approach we have investigated the use of natural lipids in the preparation of nanostructured lipid carriers (NLC). Three different NLC composed of copaiba oil and beeswax, sweet almond oil and shea butter, and sesame oil and cocoa butter as structural matrices were optimized using factorial analysis; Pluronic® 68 and lidocaine (LDC) were used as the colloidal stabilizer and model encapsulated drug, respectively. The optimal formulations were characterized by different techniques (IR-ATR, DSC, and TEM), and their safety and efficacy were also tested. These nanocarriers were able to upload high amounts of the anesthetic with a sustained in vitro release profile for 24h. The physicochemical stability in terms of size (nm), PDI, zeta potential (mV), pH, nanoparticle concentration (particles/mL), and visual inspection was followed during 12months of storage at 25°C. The formulations exhibited excellent structural properties and stability. They proved to be nontoxic in vitro (cell viability tests with Balb/c 3T3 fibroblasts) and significantly improved the in vivo effects of LDC, over the heart rate of zebra fish larvae and in the blockage of sciatic nerve in mice. The results from this study support that the proper combination of natural excipients is promising in DDS, taking advantage of the biocompatibility, low cost, and diversity of lipids.

Authors+Show Affiliations

Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil. Electronic address: nuneslica@gmail.com.Department of Analytical Chemistry, Institute of Chemistry, UNICAMP, Campinas, - São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil.Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, - São Paulo, Brazil.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28558981

Citation

Ribeiro, Lígia N M., et al. "Natural Lipids-based NLC Containing Lidocaine: From Pre-formulation to in Vivo Studies." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 106, 2017, pp. 102-112.
Ribeiro LNM, Breitkreitz MC, Guilherme VA, et al. Natural lipids-based NLC containing lidocaine: from pre-formulation to in vivo studies. Eur J Pharm Sci. 2017;106:102-112.
Ribeiro, L. N. M., Breitkreitz, M. C., Guilherme, V. A., da Silva, G. H. R., Couto, V. M., Castro, S. R., ... de Paula, E. (2017). Natural lipids-based NLC containing lidocaine: from pre-formulation to in vivo studies. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 106, pp. 102-112. doi:10.1016/j.ejps.2017.05.060.
Ribeiro LNM, et al. Natural Lipids-based NLC Containing Lidocaine: From Pre-formulation to in Vivo Studies. Eur J Pharm Sci. 2017 Aug 30;106:102-112. PubMed PMID: 28558981.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Natural lipids-based NLC containing lidocaine: from pre-formulation to in vivo studies. AU - Ribeiro,Lígia N M, AU - Breitkreitz,Márcia C, AU - Guilherme,Viviane A, AU - da Silva,Gustavo H R, AU - Couto,Verônica M, AU - Castro,Simone R, AU - de Paula,Bárbara O, AU - Machado,Daisy, AU - de Paula,Eneida, Y1 - 2017/05/27/ PY - 2017/01/09/received PY - 2017/05/25/revised PY - 2017/05/26/accepted PY - 2017/6/1/pubmed PY - 2018/12/12/medline PY - 2017/6/1/entrez KW - Beeswax KW - Nanostructured lipid carriers KW - Vegetable fats KW - Vegetable oils SP - 102 EP - 112 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 106 N2 - In a nanotechnological approach we have investigated the use of natural lipids in the preparation of nanostructured lipid carriers (NLC). Three different NLC composed of copaiba oil and beeswax, sweet almond oil and shea butter, and sesame oil and cocoa butter as structural matrices were optimized using factorial analysis; Pluronic® 68 and lidocaine (LDC) were used as the colloidal stabilizer and model encapsulated drug, respectively. The optimal formulations were characterized by different techniques (IR-ATR, DSC, and TEM), and their safety and efficacy were also tested. These nanocarriers were able to upload high amounts of the anesthetic with a sustained in vitro release profile for 24h. The physicochemical stability in terms of size (nm), PDI, zeta potential (mV), pH, nanoparticle concentration (particles/mL), and visual inspection was followed during 12months of storage at 25°C. The formulations exhibited excellent structural properties and stability. They proved to be nontoxic in vitro (cell viability tests with Balb/c 3T3 fibroblasts) and significantly improved the in vivo effects of LDC, over the heart rate of zebra fish larvae and in the blockage of sciatic nerve in mice. The results from this study support that the proper combination of natural excipients is promising in DDS, taking advantage of the biocompatibility, low cost, and diversity of lipids. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/28558981/Natural_lipids_based_NLC_containing_lidocaine:_from_pre_formulation_to_in_vivo_studies_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(17)30299-3 DB - PRIME DP - Unbound Medicine ER -