Design and evaluation of lidocaine- and prilocaine-coloaded nanoparticulate drug delivery systems for topical anesthetic analgesic therapy: a comparison between solid lipid nanoparticles and nanostructured lipid carriers

Peijun You, Ran Yuan, Chuanyu Chen, Peijun You, Ran Yuan, Chuanyu Chen

Abstract

Purpose: Topical anesthesia analgesic therapy has diverse applicability in solving the barrier properties of skin and unfavorable physicochemical properties of drugs. Lidocaine (LID) combined with prilocaine (PRI) has been used as a topical preparation for dermal anesthesia for treatment of conditions such as paresthesia.

Materials and methods: In this study, for combination anesthesia and overcoming the drawbacks of LID and PRI, respectively, LID- and PRI-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were prepared and characterized by determination of their particle size, drug loading capacity, stability, in vitro drug release behavior and in vitro cellular viability. Ex vivo skin permeation and in vivo anesthesia analgesic efficiency of these two systems were also evaluated and compared.

Results: Results revealed that combination delivery of the dual drugs exhibited more remarkable efficiency than signal drug-loaded systems. SLN systems have better ex vivo skin permeation ability than NLCs. NLC systems revealed a stronger in vivo anesthesia analgesic effect than SLN systems.

Conclusion: It can be concluded that SLNs and NLCs have different advantages, and that both carriers are promising dual drug delivery systems for topical anesthetic analgesic therapy.

Keywords: lidocaine; nanostructured lipid carriers; prilocaine; solid lipid nanoparticles; topical anesthesia.

Conflict of interest statement

Disclosure The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
The stabilities of SLNs and NLCs in terms of the mean particle diameter (A), PDI (B) and zeta potential (C). Note: Data represent the mean ± SD (n=3). Abbreviations: LID, lidocaine; NLCs, nanostructured lipid carriers; PDI, polydispersity index; PRI, prilocaine; SLNs, solid lipid nanoparticles.
Figure 2
Figure 2
In vitro LID (A) and PRI (B) release from SLN and NLC systems. Note: Data represent the mean ± SD (n=3). Abbreviations: LID, lidocaine; NLCs, nanostructured lipid carriers; PRI, prilocaine; SLNs, solid lipid nanoparticles.
Figure 3
Figure 3
In vitro cellular viability of BALB/c-3T3 fibroblast cells incubated with free drugs and drug-loaded SLN and NLC systems. Notes: Data represent the mean ± SD (n=3). *P<0.05. Abbreviations: LID, lidocaine; NLCs, nanostructured lipid carriers; PRI, prilocaine; SLNs, solid lipid nanoparticles.
Figure 4
Figure 4
Ex vivo drug permeation behaviors of LID- (A) and/or PRI-loaded (B) SLNs and NLCs and free LID and/or PRI. Note: Data represent the mean ± SD (n=6). Abbreviations: LID, lidocaine; NLCs, nanostructured lipid carriers; PRI, prilocaine; SLNs, solid lipid nanoparticles.
Figure 5
Figure 5
In vivo anesthesia analgesia effect of drug-loaded SLNs and NLCs evaluated by TF latency test. Note: Data represent the mean ± SD (n=8). Abbreviations: LID, lidocaine; NLCs, nanostructured lipid carriers; PRI, prilocaine; SLNs, solid lipid nanoparticles; TF, tail-flick.

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Source: PubMed

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