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Here, we report on the development of lipid-based nanostructures containing zidovudine (1 mg/mL) and lamivudine (0.5 mg/mL) for oral administration in the pediatric population, eliminating the use of organic solvents, which is in accordance with green chemistry principles. The formulations were obtained by ultrasonication using monoolein (MN) or phytantriol (PN), which presented narrow size distributions with similar mean particle sizes (~150 nm) determined by laser diffraction. The zeta potential and the pH values of the formulations were around -4.0 mV and 6.0, respectively. MN presented a slightly higher incorporation rate compared to PN. Nanoemulsions were obtained when using monoolein, while cubosomes were obtained when using phytantriol, as confirmed by Small-Angle X-ray Scattering. The formulations enabled drug release control and protection against acid degradation. The drug incorporation was effective and the analyses using an electronic tongue indicated a difference in palatability between the nanotechnological samples in comparison with the drug solutions. In conclusion, PN was considered to have the strongest potential as a novel oral formulation for pediatric HIV treatment.
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Psoriasis is a recurring, immune-mediated dermatological disorder. Many therapeutic agents are available for the treatment of psoriasis, including immunosuppressants and biologic treatments with immunosuppressant action. The employment of nanotechnology allows drug tailoring to achieve dermal targeting, improve efficacy and minimize undesirable effects. Here we discuss the use of the topical route in combination with nano-based drug delivery systems containing immunosuppressants for the management of psoriasis. This review is based on articles selected from 2011 to 2022, using the keywords "Psoriasis" AND "Immunosuppressants" AND "Nano*" in the main databases. Fifty-seven articles were retrieved, although only forty-two matched the inclusion criteria. Nanocarriers such as liposomes, ethosomes, niosomes, solid lipid nanoparticle, nanostructured lipid carriers and microspheres containing immunosuppressive drugs (methotrexate, cyclosporine, tacrolimus, and etanercept) were identified. The main findings of these studies are related to the improved in vitro/ex vivo permeation/penetration and therapeutic efficacy of nanoparticles in vitro and in vivo, compared to the drug in solution. Based on the studies discussed in this review, encapsulation in several types of nanocarriers decreases toxicity, dose, and dose frequency. Furthermore, it enables specific targeting of the active drug, pointing to the possibility of improving topical therapy for psoriasis. In conclusion, nanoformulations represent a novel and promising tool for psoriasis treatment.
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Nanopartículas , Psoríase , Humanos , Imunossupressores , Portadores de Fármacos , Psoríase/tratamento farmacológico , Metotrexato , NanotecnologiaRESUMO
The rose-hip oil holds skin regenerating properties with applications in the dermatological and cosmetic area. Its nanoencapsulation might favor the oil stability and its incorporation into hydrophilic formulations, besides increasing the contact with the skin and prolonging its effect. The aim of the present investigation was to develop suitable rose-hip-oil-loaded nanocapsules, to verify the nanocapsule effect on the UV-induced oxidation of the oil and to obtain topical formulations by the incorporation of the nanocapsules into chitosan gel and film. The rose-hip oil (500 or 600 µL), polymer (Eudragit RS100®, 100 or 200 mg), and acetone (50 or 100 mL) contents were separately varied aiming to obtain an adequate size distribution. The results led to a combination of the factors acetone and oil. The developed formulation showed average diameter of 158 ± 6 nm with low polydispersity, pH of 5.8 ± 0.9, zeta potential of +9.8 ± 1.5 mV, rose-hip oil content of 54 ± 1 µL/mL and tendency to reversible creaming. No differences were observed in the nanocapsules properties after storage. The nanoencapsulation of rose-hip oil decreased the UVA and UVC oxidation of the oil. The chitosan gel and film containing rose-hip-oil-loaded nanocapsules showed suitable properties for cutaneous use. In conclusion, it was possible to successfully obtain rose-hip-oil-loaded nanocapsules and to confirm the nanocapsules effect in protecting the oil from the UV rays. The chitosan gel and film were considered interesting alternatives for incorporating the nanoencapsulated rose-hip oil, combining the advantages of the nanoparticles to the advantages of chitosan.
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Hidrogéis/química , Nanocápsulas/química , Nanopartículas/química , Óleos de Plantas/química , Rosa/química , Acetona/química , Resinas Acrílicas/química , Administração Tópica , Química Farmacêutica/métodos , Quitosana/química , Tamanho da Partícula , Polímeros/química , Raios Ultravioleta/efeitos adversosRESUMO
This review is based on selected reports from 2004 to 2014 and provides a comprehensive and updated overview of the state of the art related to the drug delivery advantages of polymeric nanocapsules, which are a specific type of polymeric nanoparticles used for improvement of biological effects. Special attention is given to the application of nanocapsules to increase the chemical and photostability of drugs, to modulate the interaction with cells and tissues, to reduce adverse effects of drugs, and to increase the drug efficiency and/or bioavailability. Moreover, this review covers in vitro and in vivo studies, highlighting interesting examples of drugs from several therapeutic classes for which efficacy is improved by encapsulation in different types of nanocapsules, especially in lipid-core nanocapsules. We also briefly present the first results obtained so far attesting to the safety of using polymeric nanocapsules for drug delivery.
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Nanocápsulas/química , Preparações Farmacêuticas/química , Polímeros/química , Animais , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , HumanosRESUMO
The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit RS 100 and Eudragit S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations. Several formulations were prepared with increasing chitosan concentrations, and were analyzed in terms of pH and rheological behavior so that the most suitable formulation could be selected. The enhancement of the adhesion (tensile stress test and washability profile) and penetration (confocal laser scanning microscopy and extraction followed by quantification) properties of the formulations, when applied to porcine vaginal mucosa, were evaluated. The nanocapsule suspensions produced presented adequate properties: size of approximately 200 nm (polydispersity index of ≤0.2); zeta potential around +10 mV for the cationic formulation and -10 mV for the anionic formulation; and pH values of 6.1±0.1 (Eudragit RS 100), 5.3±0.2 (Eudragit S 100), 6.2±0.1 (Nile red loaded Eudragit RS 100), and 5.1±0.1 (Nile red loaded Eudragit S 100). The chitosan formulation presented suitable viscosity for vaginal application and acidic pH (approximately 4.5). The tensile stress test showed that both formulations containing polymeric nanocapsules presented higher mucoadhesion when compared with the formulation without nanocapsules. In the washability experiment, no significant differences were found between formulations. Confocal microscopy and fluorescence quantification after extraction from the mucosa showed higher penetration of Nile red when it was nanoencapsulated, particularly in cationic nanocapsules. The formulations developed based on chitosan gel vehicle at 2.5% weight/weight containing polymeric nanocapsules, especially the cationic nanocapsules, demonstrated applicability for the vaginal delivery of hydrophobic substances.
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Resinas Acrílicas/química , Quitosana/química , Nanocápsulas/química , Ácidos Polimetacrílicos/química , Cremes, Espumas e Géis Vaginais/química , Animais , Feminino , Modelos Biológicos , Mucosa/metabolismo , Oxazinas/química , Oxazinas/farmacocinética , Suínos , Vagina/metabolismoRESUMO
Capsaicin, a topical analgesic used in the treatment of chronic pain, has irritant properties that frequently interrupt its use. In this work, the effect of nanoencapsulation of the main capsaicinoids (capsaicin and dihydrocapsaicin) on skin irritation was tested in humans. Skin tolerance of a novel vehicle composed of chitosan hydrogel containing nonloaded nanocapsules (CH-NC) was also evaluated. The chitosan hydrogel containing nanoencapsulated capsaicinoids (CH-NC-CP) did not cause skin irritation, as measured by an erythema probe and on a visual scale, while a formulation containing free capsaicinoids (chitosan gel with hydroalcoholic solution [CH-ET-CP]) and a commercially available capsaicinoids formulation caused skin irritation. Thirty-one percent of volunteers reported slight irritation one hour after application of CH-NC-CP, while moderate (46% [CH-ET-CP] and 23% [commercial product]) and severe (8% [CH-ET-CP] and 69% [commercial product]) irritation were described for the formulations containing free capsaicinoids. When CH-NC was applied to the skin, erythema was not observed and only 8% of volunteers felt slight irritation, which demonstrates the utility of the novel vehicle. A complementary in vitro skin permeation study showed that permeation of capsaicinoids through an epidermal human membrane was reduced but not prevented by nanoencapsulation.
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Capsaicina/análogos & derivados , Capsaicina/administração & dosagem , Nanocápsulas/administração & dosagem , Administração Tópica , Adolescente , Adulto , Analgésicos não Narcóticos/administração & dosagem , Analgésicos não Narcóticos/efeitos adversos , Analgésicos não Narcóticos/farmacocinética , Capsaicina/efeitos adversos , Capsaicina/farmacocinética , Química Farmacêutica , Quitosana/química , Fármacos Dermatológicos/administração & dosagem , Fármacos Dermatológicos/efeitos adversos , Fármacos Dermatológicos/farmacocinética , Eritema/induzido quimicamente , Eritema/metabolismo , Eritema/prevenção & controle , Feminino , Humanos , Hidrogéis/química , Irritantes/administração & dosagem , Irritantes/efeitos adversos , Irritantes/farmacocinética , Masculino , Pessoa de Meia-Idade , Nanocápsulas/química , Nanomedicina , Nanotecnologia , Adulto JovemRESUMO
BACKGROUND: The incorporation of substances in nanocarriers can modulate and/or manage their delivery profiles (immediate or sustained) and permeation through skin. Consequently, drug nanencapsulation intended for topical treatment can reduce the systemic absorption of the substance. OBJECTIVE: To obtain and characterize vitamin K1-loaded lipid core nanocapsules as well as to determine whether the nanoencapsulation influences the skin permeation of this vitamin. METHODS: The skin permeation study was performed by means of Franz-type diffusion cells followed by the tape stripping and retention techniques. The vitamin K1-loaded lipid core nanocapsules were obtained by the preformed polymer precipitation method and the particles were characterized. RESULTS: The nanocapsules presented average diameter of 211 ± 2 nm, pH of 5.7 ± 0.3, zeta potential of -14.9 ± 0.6 mV and drug content of 10.2 mg/mL (102.1%). The physical stability of the nanocapsule suspension was verified using multiple light backscattering analysis. The amount of vitamin K1 in the dermis after 8 h of drug permeation was higher when the nanocapsules were applied compared to the control. Moreover, retention in the outermost skin layer and a decrease in the skin permeation to the receptor compartment due to the nanoencapsulation were observed. CONCLUSION: Thus, nanoencapsulation can lead to the selective permeation of vitamin K1 through the skin.
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Portadores de Fármacos/farmacocinética , Nanocápsulas/química , Pele/metabolismo , Vitamina K 1/farmacocinética , Vitaminas/farmacocinética , Animais , Portadores de Fármacos/química , Feminino , Técnicas In Vitro , Lipídeos/química , Tamanho da Partícula , Polímeros/química , Polímeros/farmacocinética , Absorção Cutânea , Suínos , ViscosidadeRESUMO
INTRODUCTION: The cosmetic benefit obtained from the use of lipoic acid in the treatment of different skin disorders related to oxidative stress is compromised by its chemical instability, which complicates the preparation of cosmetic formulations suitable for topical use. Considering that nanoencapsulation increases the stability of lipoic acid, the aim of this study was to develop different semisolid formulations, based on innovative cosmetic ingredients and containing lipoic acid-loaded nanocapsules. MATERIALS AND METHODS: Lipoic acid-loaded nanocapsules (5.0 mg/mL) were prepared by interfacial deposition of the pre-formed polymer and the thickening agents Aristoflex AVC and DC RM2051, used alone or in combination. The formulations were characterized in terms of resistance to centrifugation, pH, lipoic acid content, rheological characteristics and optical parameters determined by multiple light scattering. Also, their stability when subjected to cycles of thermal heating and freezing was evaluated. RESULTS AND DISCUSSION: The semisolid formulations presented suitable properties for cutaneous administration, with enhanced physicochemical stability, considering the drug content and resistance to centrifugation, being observed for the formulations containing nanocapsules. All of the proposed formulations showed pseudoplastic flow behavior. The nanoencapsulation leads to an increase in the flow indexes. After the stress cycles an improvement in the consistency, particularly for the formulations containing nanocapsules, was observed. According to the results of multiple light scattering analysis, the formulations can be considered stable. CONCLUSIONS: The use of new cosmetic ingredients, unlike traditional hydrogels, represents a differentiated platform for preparation of stable semisolid formulations containing polymeric nanocapsules, presenting physicochemical properties suitable for topical use.