Strategies for delivering local anesthetics to the skin: focus on liposomes, solid lipid nanoparticles, hydrogels and patches

Araújo, Daniele Ribeiro de; Silva, Deyse C. da; Barbosa, Raquel de Melo; Franz-Montan, Michelle; Cereda, Cíntia Maria Saia; Padula, Cristina; Santi, Patrizia; Paula, Eneida de

doi:10.1517/17425247.2013.828031

Cited by 61 publications

(35 citation statements)

References 104 publications

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“…Their highly porous structure can easily be tuned by controlling the density of cross-links in the gel matrix and the affinity of the HG for the aqueous environment in which they are swollen (8,9). By modifying the HG density, the rate at which an entrapped drug is released can be altered to allow the delivery of the drug over a specific period (10). Concretely, micro/ nanostructured polymeric systems have attracted much attention because of their pharmaceutical applications.…”

Section: Introductionmentioning

confidence: 99%

Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels

et al. 2017

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In order to obtain dermal vehicles of ketorolac tromethamine (KT) for the local treatment of inflammation and restrict undesirable side effects of systemic levels hydrogels (HGs) of poloxamer and carbomer were developed. METHODS:KT poloxamer based HG (KT-P407-HG) and KT carbomer based HG (KT-C940-HG) were elaborated and characterized in terms of swelling, degradation, porosity, rheology, stability, in vitro release, ex vivo permeation and distribution skin layers. Finally, in vivo anti-inflammatory efficacy and skin tolerance were also assessed. RESULTS:HGs were transparent and kept stable after 3 months exhibiting biocompatible near neutral pH values. Rheological patterns fitted to Herschel-Bulkley for KT-C940-HG and Newton for KT-P407-HG due to its low viscosity at 25°C. Rapid release profiles were observed through first order kinetics. Following the surface the highest concentration of KT from C940-HG was found in the epidermis and the stratum corneum for P407-HG. Relevant anti-inflammatory efficacy of KT-P407-HG revealed enough ability to provide sufficient bioavailability KT to reach easily the site of action. The application of developed formulations in volunteers did not induce any visual skin irritation. CONCLUSIONS:KT-P407-HG was proposed as suitable formulation for anti-inflammatory local treatment without theoretical systemic side effect.

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Section: Introductionmentioning

confidence: 99%

Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels

et al. 2017

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“…The condition of analgesia is mostly achieved through direct intradermal injection of local anaesthetic drugs which causes much discomfort (1). Injections of local anaesthetics are painful which in turn cause tissue oedema and distortion of the surgical site (2).…”

Section: Introductionmentioning

confidence: 99%

Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia

et al. 2016

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The topical delivery of local anaesthetics has always been a difficult task due to the limited percutaneous absorption of local anaesthetic drugs across the various barriers of the skin. In this pursuit, a thermoresponsive mixed micellar nanogel (MMNG) system of lidocaine and prilocaine has been attempted in the current piece of work. The system relies on the ability to alter its phase state (sol-to-gel) for feasibility of the topical application in response to change in temperature. The composition of MMNG entails majorly of Pluronic® F127 and Tween 80 in a fixed combination so as to provide the desired thermoreversibility for the skin application. The gels were optimized with respect to phase transition temperature (T ), turbidity and viscosity. The optimized systems were then characterized for particle size, spreadability, syringeability, bioadhesive strength, ex vivo skin permeation, retention and dermatokinetic studies. The skin compatibility revealed that no histological changes were observed for optimized formulation, while the conventional system showed changes in the skin-tissues. Further, the enhanced intensity of anaesthetic effect was noted in an in vivo rabbit model and tail flick model in mice. The overall results suggest that the prepared MMNG system possesses the potential in providing an efficacious, safe and acceptable alternative therapeutic system for topical anaesthesia.

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“…Nowadays, the development of local anesthetics skin-delivery systems using liposomes (LPs) or lipid nanoparticles have been explored as alternatives to commercial formulations such as lidocaine and prilocaine cream (EMLA Õ , Astra Zeneca), lidocaine tape (Penles Õ , Wyeth) or lidocaine gel path (Lidoderm Õ , Endo Pharmaceuticals), modifying the release rate of drugs, increasing bioadhesive properties and reducing toxicity, resulting in an improved therapeutic efficacy (Houck et al, 2005;de Araújo et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

An alternative choice of lidocaine-loaded liposomes: lidocaine-loaded lipid–polymer hybrid nanoparticles for local anesthetic therapy

et al. 2016

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Purpose: The skin permeation enhancement of local anesthetics by newer innovative nanotechnologies has been an appealing field recently. However, which nanocarrier is better for drug loading and has better stability? Therefore, the aim of our study was to compare two kinds of nanocarriers: liposomes and lipid-polymer hybrid nanoparticles (LPNs) for lidocaine (LA) delivery. Methods: LA-loaded liposomes (LA-LPs) and LPNs (LA-LPNs) were prepared. Two kinds of nanocarriers were characterized in terms of particle size, zeta potential, drug encapsulation efficiency (EE), drug release, and stability. Their in vitro skin permeation was studied using a Franz diffusion cell mounted with depilated mouse skin in vitro. In vivo local anesthetic effects of LA containing formulations were evaluated by tail flick latency (TFL) test using a tail-flick measuring device. Results: Compared with LA-LPs, LA-LPNs showed significantly better in vitro skin permeation ability and in vivo local anesthetic effects. Conclusion:The results demonstrated that LPNs could improve the efficacy of drugs to higher levels than LPs and free drugs, thus could serve as an effective drug system for LA loading for local anesthetic therapy.

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Strategies for delivering local anesthetics to the skin: focus on liposomes, solid lipid nanoparticles, hydrogels and patches

Cited by 61 publications

References 104 publications

Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels

Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels

Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia

An alternative choice of lidocaine-loaded liposomes: lidocaine-loaded lipid–polymer hybrid nanoparticles for local anesthetic therapy

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