Monoketonic Curcuminoid-Lidocaine Co-Deliver Using Thermosensitive Organogels: From Drug Synthesis to Epidermis Structural Studies

Vigato, Aryane Alves; Machado, Isabel Daufenback; Valle, Matheus del; Ana, Patrícia Aparecida; Sepulveda, Anderson Ferreira; Yokaichiya, Fabiano; Franco, Margareth K. K. D.; Loiola, Messias C.; Tófoli, Giovana Radomille; Cereda, Cíntia Maria Saia; Sairre, Mirela Inês de; Araújo, Daniele Ribeiro de

doi:10.3390/pharmaceutics14020293

Cited by 12 publications

(10 citation statements)

References 67 publications

(95 reference statements)

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“…3 B) showed that the emulsion and PCL alone exhibited more of a liquid character than the gel formulations, considered to be pseudoplastic behavior. This pseudoplastic character shows that the gel reduces materials outflow, a favorable indicator for topical applications [ 39 , 40 , 52 , 53 ] as repellents must remain on the skin surface at the application site.…”

Section: Resultsmentioning

confidence: 99%

“…The elastic Gʹ and viscous moduli G" were measured between 0 and 60 °C. Gʹ and G" measurements were also made with ω frequency from 0.1 to 10 Hz at 32.5 °C [ 39 ]. The flow curves σ (γ ˙) (“backward” and “forward”) were obtained at 32.5 °C with a shear rate γ ˙ ranging from 0 to 100 s −1 .…”

Section: Methodsmentioning

confidence: 99%

“…Epidermis samples were stored at − 20 °C for a maximum of 3 months. For structural analysis, the epidermis surface (0.8 cm diameter) was treated with repellent formulations and kept in contact for 24 h at room temperature [ 39 ]. Formulations were then removed from the epidermis samples and analyzed by FTIR.…”

Section: Methodsmentioning

confidence: 99%

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Repellent active ingredients encapsulated in polymeric nanoparticles: potential alternative formulations to control arboviruses

et al. 2022

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Dengue, yellow fever, Chinkungunya, Zika virus, and West Nile fever have infected millions and killed a considerable number of humans since their emergence. These arboviruses are transmitted by mosquito bites and topical chemical repellents are the most commonly used method to protect against vector arthropod species. This study aimed to develop a new generation of repellent formulations to promote improved arboviruses transmission control. A repellent system based on polycaprolactone (PCL)-polymeric nanoparticles was developed for the dual encapsulation of IR3535 and geraniol and further incorporation into a thermosensitive hydrogel. The physicochemical and morphological parameters of the prepared formulations were evaluated by dynamic light scattering (DLS), nano tracking analysis (NTA), atomic force microscopy (AFM). In vitro release mechanisms and permeation performance were evaluated before and after nanoparticles incorporation into the hydrogels. FTIR analysis was performed to evaluate the effect of formulation epidermal contact. Potential cytotoxicity was evaluated using the MTT reduction test and disc diffusion methods. The nanoparticle formulations were stable over 120 days with encapsulation efficiency (EE) of 60% and 99% for IR3535 and geraniol, respectively. AFM analysis revealed a spherical nanoparticle morphology. After 24 h, 7 ± 0.1% and 83 ± 2% of the GRL and IR3535, respectively, were released while the same formulation incorporated in poloxamer 407 hydrogel released 11 ± 0.9% and 29 ± 3% of the loaded GRL and IR3535, respectively. GRL permeation from PCL nanoparticles and PCL nanoparticles in the hydrogel showed similar profiles, while IR3535 permeation was modulated by formulation compositions. Differences in IR3535 permeated amounts were higher for PCL nanoparticles in the hydrogels (36.9 ± 1.1 mg/cm2) compared to the IR3535-PCL nanoparticles (29.2 ± 1.5 mg/cm2). However, both active permeation concentrations were low at 24 h, indicating that the formulations (PCL nanoparticles and PCL in hydrogel) controlled the bioactive percutaneous absorption. Minor changes in the stratum corneum (SC) caused by interaction with the formulations may not represent a consumer safety risk. The cytotoxicity results presented herein indicate the carrier systems based on poly-epsilon caprolactone (PCL) exhibited a reduced toxic effect when compared to emulsions, opening perspectives for these systems to be used as a tool to prolong protection times with lower active repellent concentrations.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Repellent active ingredients encapsulated in polymeric nanoparticles: potential alternative formulations to control arboviruses

et al. 2022

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“…However, the studies on dynamics of polydisperse emulsions transport through microchannels and the development of complex models of The first case, known as "slug flow", is widely reported in the literature [14][15][16]. The analysis of the individual droplets transport, their deformation, and tearing in channels with a similar diameter, has gained particular interest within the formation of monodisperse emulsions, in various types of droplet generators [17,18]. The knowledge of the flow dynamics and the interactions between the phases and the channel wall proved to be extremely important for obtaining droplets of specific sizes [19].…”

Section: Introductionmentioning

confidence: 99%

The Phenomenon of Drug Emulsion Carriers Compaction during Their Movement in Microstructures

2022

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The greatest challenges of modern pharmacology are the design of drugs with the highest possible efficacy of an active substance and with the lowest possible invasiveness for the whole organism. A good solution features the application of a bioactive substance in different carriers. The effectiveness of such preparations is determined not only by the properties of the drug, but primarily by the dynamics of carrier movement in the body. This is the reason why studies on the dispersed systems transport in micro- and nanostructures are becoming important. This paper presents a study of emulsion systems transport in microcapillaries. A dispersed phase thickening effect was observed during the process, which resulted in a concentration increase of the flowing emulsion, in some cases up to 10 times. This phenomenon directly influences transport dynamics of such substances in microstructures and should be taken into account when designing drug parameters (concentration, release time, and action range). The effect was investigated for three different emulsions concentrations and presented quantitatively. The scales of this phenomenon occurrence at different flow conditions were investigated, and their magnitudes were modelled and described. This allows the prediction of the flow resistance in the movement of given dispersion systems, as a function of the flow rate, the emulsion parameters, and the microchannel size.

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“…Nanoscale drug delivery systems (DDS) have been designed as inert systems that can transport drugs at the target site with high selectivity and controllable kinetic release profile [ 6 , 7 ]. Various DDS, such as niosomes, liposomes, transferosomes, and solid lipid nanoparticles, have already been employed to improve LID efficacy due to the role of these systems as skin permeation enhancers able to increase drug permeability, and consequently, ensure a higher drug accumulation at the target site and thus, an improved analgesic effect [ 8 , 9 , 10 , 11 ]. Their better permeation ability allows for lower drug doses and could reduce cardiovascular side effects [ 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

Lidosomes: Innovative Vesicular Systems Prepared from Lidocaine Surfadrug

Romeo

Mazzotta²,

Perrotta³

et al. 2022

Pharmaceutics

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Lidocaine is a local anaesthetic drug with an amphiphilic structure able to self-associate, under certain conditions, in molecular aggregates playing the role of both carrier and drug. The aim of this study was to determine the optimal conditions for obtaining vesicular carriers, called lidosomes. The new formulations were obtained using both lidocaine and lidocaine hydrochloride and different hydration medias (distilled water, acid, and basic aqueous solution). Lidosomes formulations were characterized in terms of size, ζ-potential, drug retained, stability formulation, and ex vivo permeation profile. Moreover, lidosomes were incorporated in two different gel structures: one based on carboxymethylcellulose and one based on pluronic F-127 to achieve suitable properties for a topical application. Results obtained showed that lidocaine showed a better performance to aggregate in vesicular carriers in respect to hydrochloride form. Consequently, only formulations comprised of lidocaine were studied in terms of skin permeation performance and as carriers of another model drug, capsaicin, for a potential combined therapy. Lidocaine, when in form of vesicular aggregates, acted as percutaneous permeation enhancer showing better permeation profiles with respect to drug solutions. Moreover, lidosomes created a significant drug depot into the skin from which the drug was available for a prolonged time, a suitable feature for a successful local therapy.

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Monoketonic Curcuminoid-Lidocaine Co-Deliver Using Thermosensitive Organogels: From Drug Synthesis to Epidermis Structural Studies

Cited by 12 publications

References 67 publications

Repellent active ingredients encapsulated in polymeric nanoparticles: potential alternative formulations to control arboviruses

Repellent active ingredients encapsulated in polymeric nanoparticles: potential alternative formulations to control arboviruses

The Phenomenon of Drug Emulsion Carriers Compaction during Their Movement in Microstructures

Lidosomes: Innovative Vesicular Systems Prepared from Lidocaine Surfadrug

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