Benzocaine loaded biodegradable poly-(d,l-lactide-co-glycolide) nanocapsules: factorial design and characterization

Moraes, Carolina Morales; Matos, Angélica Prado de; Paula, Eneida de; Rosa, André Henrique; Fraceto, Leonardo Fernandes

doi:10.1016/j.mseb.2009.06.011

Cited by 35 publications

(35 citation statements)

References 27 publications

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“…4,5,52 The BVC association rate in the PLGA nanocapsules was 75.8%, which is a very high value when compared to other studies reported in the literature for local anesthetics. [44][45][46][47][48] The stabilities of the NC polymer suspensions containing BVC were evaluated based on the physicochemical properties of size, polydispersity, zeta potential and association efficiency as a function of time (initial, 15, 60 and 120 days), with all the samples stored in amber glass flasks at room temperature.…”

Section: Resultsmentioning

confidence: 99%

“…[44][45][46][47][48] The stabilities of the NC polymer suspensions containing BVC were evaluated based on the physicochemical properties of size, polydispersity, zeta potential and association efficiency as a function of time (initial, 15, 60 and 120 days), with all the samples stored in amber glass flasks at room temperature.…”

Section: 552mentioning

confidence: 99%

“…20 The delivery of local anesthetics, which has been studied extensively by many research groups and also by our laboratory, can be achieved by the formation of inclusion complexes with cyclodextrins, 20-30 encapsulation in liposomes, [31][32][33][34][35][36][37][38][39] association to polymer microparticles [40][41][42][43] and association to polymeric nanostructured systems. [44][45][46][47][48] The use of colloidal systems of polymeric nanoparticles is often limited due to problems of stability over long periods of time. A colloidal suspension does not normally show phase separation, since both sedimentation and aggregate formation are slow.…”

Section: Introductionmentioning

confidence: 99%

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Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

Moraes

Paula

Rosa

et al. 2010

J. Braz. Chem. Soc.

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Neste trabalho foi realizada a preparação de nanocápsulas de poli (DL-lactídeo-co-glicolídeo) (PLGA) como um sistema carreador para o anestésico local bupivacaína. A preparação foi caracterizada e sua estabilidade físico-química avaliada. Os resultados da caracterização mostram uma distribuição de tamanho com um índice de polidispersão de 0,12, um diâmetro médio de 148 nm, um potencial zeta de -43,5 mV e uma eficiência de associação da BVC nas nanocápsulas de 75,8%. As propriedades físico-químicas das suspensões (diâmetro hidrodinâmico, índice de polidispersão, potencial zeta e eficiência de associação do fármaco) contendo nanocápsulas poliméricas foram avaliadas em função do tempo a fim de determinar sua estabilidade. Nenhuma grande alteração foi observada em função tempo para as suspensões de nanocápsulas avaliadas, sendo consideradas estáveis por um período de armazenagem de 120 dias a temperatura ambiente. Os resultados aqui apresentados, os quais se referem ao estudo desta nova formulação para anestésico local bupivacaína mostram-se promissores para futuros estudos in vivo.This paper describes the preparation of poly(DL-lactide-co-glicolide) (PLGA) nanocapsules as a drug carrier system for the local anesthetic bupivacaine. The system was characterized and its stability investigated. The results showed a size distribution with a polydispersity index of 0.12, an average diameter of 148 nm, a zeta potential of -43.5 mV and an entrapment efficiency of 75.8%. The physicochemical properties of polymeric nanocapsule suspensions (average diameter, polydispersity, zeta potential and drug association efficiency) were evaluated as a function of time to determine the formulation stability. The formulation did not display major changes in these properties over the time, and it was considered stable up to 120 days of storage at room temperature. The results reported here which refer to the initial characterization of these new formulations for the local anesthetic bupivacaine show a promising potential for future in vivo studies.Keywords: bupivacaine, local anesthetic, polymeric nanocapsules, PLGA, physical-chemical stability IntroductionNumerous studies today are focusing on the development of new pharmaceutical formulations based on nanocarriers, which have demonstrated several advantages over conventional formulations, making this research line a promising and innovative area of the pharmaceutical sector. 1,2Polymer nanoparticles (PN) are carriers of drugs or other active molecules whose sizes range from 10 to 1000 nm. Nanospheres (NS) or nanocapsules (NC) can be obtained, depending on the method of preparation and the materials employed. NC consists of a polymer casing and a nucleus (usually oily). The drug inside the NC may be dissolved in the oily nucleus or adsorbed on the polymeric wall. NS, on the other hand, consists of a polymer matrix and their composition does not include oil. In this system, the drug may be adsorbed or dispersed in the polymeric matrix. [2][3][4][5][6] Several polymers are used in the prepa...

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Section: Resultsmentioning

confidence: 99%

Section: 552mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

Moraes

Paula

Rosa

et al. 2010

J. Braz. Chem. Soc.

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“…Features such as lack of toxicity, high physical stability and affinity for the active ingredient are important characteristics of the NE oil core that should be considered (Moraes et al, 2009). …”

Section: Vegetable Oils In Nanoemulsionsmentioning

confidence: 99%

The use of Brazilian vegetable oils in nanoemulsions: an update on preparation and biological applications

Bajerski

Michels

Colomé

et al. 2016

Braz. J. Pharm. Sci.

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Vegetable oils present important pharmacological properties, which gained ground in the pharmaceutical field. Its encapsulation in nanoemulsions is considered a promising strategy to facilitate the applicability of these natural compounds and to potentiate the actions. These formulations offer several advantages for topical and systemic delivery of cosmetic and pharmaceutical agents including controlled droplet size, protection of the vegetable oil to photo, thermal and volatilization instability and ability to dissolve and stabilize lipophilic drugs. For these reasons, the aim of this review is to report on some characteristics, preparation methods, applications and especially analyze recent research available in the literature concerning the use of vegetable oils with therapeutic characteristics as lipid core in nanoemulsions, specially from Brazilian flora, such as babassu (Orbignya oleifera), aroeira (Schinus molle L.), andiroba (Carapa guaianiensis), casca-de-anta (Drimys brasiliensis Miers), sucupira (Pterodon emarginatus Vogel) and carqueja doce (Stenachaenium megapotamicum) oils.Uniterms: Plant oils/nanoemulsions/preparation. Plant oils/biological applications. INTRODUCTIONThe use of submicrometric colloidal nanocarriers such as nanoparticles (NP) lipid and polymeric, nanoemulsions (NE), microemulsions (ME), liposomes, and polymeric micelles is considered a promising system in the pharmaceutical field, because they have numerous advantages over traditional formulations such as: sustained release of the active element; solubilization of lipophilic molecules; use for different routes of administration; protection from chemical and enzymatic degradation of labile molecules; reduction of vegetable oils (VO) volatilization, side effects and dose (Mäder, Mehnert, 2005;Mehnert, Mäder, 2001;Gref, Couvreour, 2006;Couvreur, Vauthier, 2006; Panyam, Labhasetwar, 2003;Soppimath et al., 2001;Ai et al., 2011; Contri et al., 2012;Contri et al., 2014;Dimer et al., 2014;Severino et al., 2015;Frank et al., 2015;Asbahani et al., 2015). However, all systems differ thermodynamic stability, structure, chemical composition, efficiency encapsulation and types of application (Mäder, Mehnert, 2005;Ai et al., 2011).The development of suitable nanocarriers for pharmaceutical or cosmetic application requires the adequate selection of their adjuvants such as polymers for nanocapsules (NC), surfactants, and oils (Schaffazick et al., 2003;Alvarez-Román et al., 2001;Bouchemal et al., 2004;Friedrich et al., 2008). Recently, special attention has been given to the type of oily phase used as the core in the preparation of NE. VO has been preferred not only due to the concept that it is safe and biocompatible, but mainly because of the diversity of benefits, and the complex composition of fatty acids can exercise under the skin, protecting it against dehydration, solar radiation, inflammation, insect attack, microorganisms, and viruses (Tadros, Kessell, 2004;Bloise, 2003;Oyedeji, Okeke, 2010;Bakkali et. al., 2008;Harris, 2002; Contri et al, ...

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“…[100][101][102] This method consists in creating an organic phase composed of the drug (benzocaine in all reported works), the polymer, acetone, oil, and the emulsifier. The organic phase is mixed under magnetic stirring with an aqueous solution containing an emulsifier in turn, and acetone is evaporated by rotary evaporation.…”

Section: Nanostructured Systemsmentioning

confidence: 99%

From micro- to nanostructured implantable device for local anesthetic delivery

Zorzetto

Brambilla

Marcello

et al. 2016

IJN

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Local anesthetics block the transmission of painful stimuli to the brain by acting on ion channels of nociceptor fibers, and find application in the management of acute and chronic pain. Despite the key role they play in modern medicine, their cardio and neurotoxicity (together with their short half-life) stress the need for developing implantable devices for tailored local drug release, with the aim of counterbalancing their side effects and prolonging their pharmacological activity. This review discusses the evolution of the physical forms of local anesthetic delivery systems during the past decades. Depending on the use of different biocompatible materials (degradable polyesters, thermosensitive hydrogels, and liposomes and hydrogels from natural polymers) and manufacturing processes, these systems can be classified as films or micro- or nanostructured devices. We analyze and summarize the production techniques according to this classification, focusing on their relative advantages and disadvantages. The most relevant trend reported in this work highlights the effort of moving from microstructured to nanostructured systems, with the aim of reaching a scale comparable to the biological environment. Improved intracellular penetration compared to microstructured systems, indeed, provides specific drug absorption into the targeted tissue and can lead to an enhancement of its bioavailability and retention time. Nanostructured systems are realized by the modification of existing manufacturing processes (interfacial deposition and nanoprecipitation for degradable polyester particles and high- or low-temperature homogenization for liposomes) or development of novel strategies (electrospun matrices and nanogels). The high surface-to-volume ratio that characterizes nanostructured devices often leads to a burst drug release. This drawback needs to be addressed to fully exploit the advantage of the interaction between the target tissues and the drug: possible strategies could involve specific binding between the drug and the material chosen for the device, and a multiscale approach to reach a tailored, prolonged drug release

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Benzocaine loaded biodegradable poly-(d,l-lactide-co-glycolide) nanocapsules: factorial design and characterization

Cited by 35 publications

References 27 publications

Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

The use of Brazilian vegetable oils in nanoemulsions: an update on preparation and biological applications

From micro- to nanostructured implantable device for local anesthetic delivery

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