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Benzocaine loaded solid lipid nanoparticles: Formulation design, in vitro and in vivo evaluation of local anesthetic effect.
Curr Drug Deliv 2015; 12(6):680-92CD

Abstract

The aim of the present work is the development and evaluation of solid lipid nanoparticles (SLNs) as carrier system for topical delivery of benzocaine (BZC) improving its local anesthesia aiming to produce a fast acting and long lasting topical formulation. BZC loaded SLNs were prepared using a full factorial design to study the influence of the type of polyoxyethylene sorbitan ester surfactants as well as their concentration as independent variables on the particle size, entrapment efficacy and zeta potential selected as dependent variables. Design of experiment (DOE) and the analysis of variance (ANOVA) were conducted to assess the optimization of the developed formulations. The results indicated that the fatty acid chain length of tested surfactants and their concentration had a significant effect on the studied responses. The optimized formulations were spherical in shape of mean particle diameters<350 nm with negatively charged surface <-20mV. Particles were characterized using differential scanning calorimetry and X-ray powder diffraction confirming the amorphous nature and the uniformity of drug inclusion in the lipid matrix. Optimized BZC-SLNs were incorporated into hydrogels characterized by a pseudoplastic non-Newtonian behavior. In vitro release study revealed an apparently biphasic release process with sustained release profile following Higuchi kinetics. BZC loaded SLNs hydrogels showed more potent anesthetic effect compared to BZC hydrogel evaluated using tail-flick analgesimeter, confirming significant improvement in both the intensity and duration of anesthetic effect. The above results proved that SLNs represent good candidates to encapsulate BZC improving its therapeutic efficacy for the topical treatment of pain.

Authors+Show Affiliations

Pharmaceutical Technology Department, National Research Centre, Cairo, 12622 Egypt. mona-basha@hotmail.com.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26138680

Citation

Basha, Mona, et al. "Benzocaine Loaded Solid Lipid Nanoparticles: Formulation Design, in Vitro and in Vivo Evaluation of Local Anesthetic Effect." Current Drug Delivery, vol. 12, no. 6, 2015, pp. 680-92.
Basha M, Abd El-Alim SH, Kassem AA, et al. Benzocaine loaded solid lipid nanoparticles: Formulation design, in vitro and in vivo evaluation of local anesthetic effect. Curr Drug Deliv. 2015;12(6):680-92.
Basha, M., Abd El-Alim, S. H., Kassem, A. A., El Awdan, S., & Awad, G. (2015). Benzocaine loaded solid lipid nanoparticles: Formulation design, in vitro and in vivo evaluation of local anesthetic effect. Current Drug Delivery, 12(6), pp. 680-92.
Basha M, et al. Benzocaine Loaded Solid Lipid Nanoparticles: Formulation Design, in Vitro and in Vivo Evaluation of Local Anesthetic Effect. Curr Drug Deliv. 2015;12(6):680-92. PubMed PMID: 26138680.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Benzocaine loaded solid lipid nanoparticles: Formulation design, in vitro and in vivo evaluation of local anesthetic effect. AU - Basha,Mona, AU - Abd El-Alim,Sameh Hosam, AU - Kassem,Ahmed Alaa, AU - El Awdan,Sally, AU - Awad,Gamal, PY - 2015/04/07/received PY - 2015/06/10/revised PY - 2015/06/20/accepted PY - 2015/7/4/entrez PY - 2015/7/4/pubmed PY - 2016/9/27/medline SP - 680 EP - 92 JF - Current drug delivery JO - Curr Drug Deliv VL - 12 IS - 6 N2 - The aim of the present work is the development and evaluation of solid lipid nanoparticles (SLNs) as carrier system for topical delivery of benzocaine (BZC) improving its local anesthesia aiming to produce a fast acting and long lasting topical formulation. BZC loaded SLNs were prepared using a full factorial design to study the influence of the type of polyoxyethylene sorbitan ester surfactants as well as their concentration as independent variables on the particle size, entrapment efficacy and zeta potential selected as dependent variables. Design of experiment (DOE) and the analysis of variance (ANOVA) were conducted to assess the optimization of the developed formulations. The results indicated that the fatty acid chain length of tested surfactants and their concentration had a significant effect on the studied responses. The optimized formulations were spherical in shape of mean particle diameters<350 nm with negatively charged surface <-20mV. Particles were characterized using differential scanning calorimetry and X-ray powder diffraction confirming the amorphous nature and the uniformity of drug inclusion in the lipid matrix. Optimized BZC-SLNs were incorporated into hydrogels characterized by a pseudoplastic non-Newtonian behavior. In vitro release study revealed an apparently biphasic release process with sustained release profile following Higuchi kinetics. BZC loaded SLNs hydrogels showed more potent anesthetic effect compared to BZC hydrogel evaluated using tail-flick analgesimeter, confirming significant improvement in both the intensity and duration of anesthetic effect. The above results proved that SLNs represent good candidates to encapsulate BZC improving its therapeutic efficacy for the topical treatment of pain. SN - 1875-5704 UR - https://www.unboundmedicine.com/medline/citation/26138680/Benzocaine_loaded_solid_lipid_nanoparticles:_Formulation_design_in_vitro_and_in_vivo_evaluation_of_local_anesthetic_effect_ L2 - http://www.eurekaselect.com/132774/article DB - PRIME DP - Unbound Medicine ER -