RESUMO
Micro-emulsions and sometimes nano-emulsions are well known candidates to deliver drugs locally. However, the poor rheological properties are marginally affecting their acceptance pharmaceutically. This work aimed to modify the poor flow properties of a nano-scaled emulsion comprising palm olein esters as the oil phase and ibuprofen as the active ingredient for topical delivery. Three Carbopol ® resins: 934, 940 and Ultrez 10, were utilized in various concentrations to achieve these goals. Moreover, phosphate buffer and triethanolamine solutions pH 7.4 were used as neutralizing agents to assess their effects on the gel-forming and swelling properties of Carbopol ® 940. The addition of these polymers caused the produced nano-scaled emulsion to show a dramatic droplets enlargement of the dispersed globules, increased intrinsic viscosity, consistent zeta potential and transparent-to-opaque change in appearance. These changes were relatively influenced by the type and the concentration of the resin used. Carbopol ® 940 and triethanolamine appeared to be superior in achieving the proposed tasks compared to other materials. The higher the pH of triethanolamine solution, the stronger the flow-modifying properties of Carbopol ® 940. Transmission electron microscopy confirmed the formation of a well-arranged gel network of Carbopol ® 940, which was the major cause for all realized changes. Later in vitro permeation studies showed a significant decrease in the drug penetration, thus further modification using 10% w/w menthol or limonene as permeation promoters was performed. This resulted in in vitro and in vivo pharmacodynamics properties that are comparably higher than the reference chosen for this study.
Assuntos
Acrilatos/química , Resinas Acrílicas/química , Anti-Inflamatórios não Esteroides/química , Portadores de Fármacos , Ésteres/química , Excipientes/química , Ibuprofeno/química , Nanopartículas , Óleos de Plantas/química , Administração Cutânea , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/farmacocinética , Soluções Tampão , Química Farmacêutica , Cicloexenos/química , Cicloexenos/farmacologia , Emulsões , Etanolaminas/química , Concentração de Íons de Hidrogênio , Ibuprofeno/administração & dosagem , Ibuprofeno/farmacocinética , Limoneno , Mentol/química , Mentol/farmacologia , Microscopia Eletrônica de Transmissão , Nanotecnologia , Óleo de Palmeira , Tamanho da Partícula , Permeabilidade , Ratos , Ratos Wistar , Reologia , Pele/efeitos dos fármacos , Pele/metabolismo , Absorção Cutânea , Propriedades de Superfície , Tecnologia Farmacêutica/métodos , Terpenos/química , Terpenos/farmacologia , ViscosidadeRESUMO
The surface activity of some non-steroidal anti-inflammatory agents like ibuprofen was investigated extensively. This fact has attracted the researchers to extend this behavior to other agents like piroxicam. Piroxicam molecules are expected to orient at the interface of oil and aqueous phase. The aim of this study was, firstly, to assess the surface and interfacial tension behaviour of newly synthesised palm oil esters and various pH phosphate buffers. Furthermore, the surface and interfacial tension activity of piroxicam was studied. All the measurements of surface and interfacial tension were made using the tensiometer. The study revealed that piroxicam has no effect on surface tension values of all pH phosphate buffers and palm oil esters. Similarly, various concentrations of piroxicam did not affect the interfacial tensions between the oil phase and the buffer phases. Accordingly, the interfacial tension values of all mixtures of oil and phosphate buffers were considerably high which indicates the immiscibility. It could be concluded that piroxicam has no surface activity. Additionally, there is no surface pressure activity of piroxicam at the interface of plam oil esters and phosphate buffers in the presence of Tweens and Spans.
Assuntos
Anti-Inflamatórios não Esteroides/química , Piroxicam/química , Humanos , Concentração de Íons de Hidrogênio , Óleo de Palmeira , Óleos de Plantas/química , Tensão SuperficialRESUMO
BACKGROUND: Recently there has been a remarkable surge of interest about natural products and their applications in the cosmetic industry. Topical delivery of antioxidants from natural sources is one of the approaches used to reverse signs of skin aging. The aim of this research was to develop a nanoemulsion cream for topical delivery of 30% ethanolic extract derived from local Phyllanthus urinaria (P. urinaria) for skin antiaging. METHODS: Palm kernel oil esters (PKOEs)-based nanoemulsions were loaded with P. urinaria extract using a spontaneous method and characterized with respect to particle size, zeta potential, and rheological properties. The release profile of the extract was evaluated using in vitro Franz diffusion cells from an artificial membrane and the antioxidant activity of the extract released was evaluated using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) method. RESULTS: Formulation F12 consisted of wt/wt, 0.05% P. urinaria extract, 1% cetyl alcohol, 0.5% glyceryl monostearate, 12% PKOEs, and 27% Tween 80/Span 80 (9/1) with a hydrophilic lipophilic balance of 13.9, and a 59.5% phosphate buffer system at pH 7.4. Formulation F36 was comprised of 0.05% P. urinaria extract, 1% cetyl alcohol, 1% glyceryl monostearate, 14% PKOEs, 28% Tween 80/Span 80 (9/1) with a hydrophilic lipophilic balance of 13.9, and 56% phosphate buffer system at pH 7.4 with shear thinning and thixotropy. The droplet size of F12 and F36 was 30.74 nm and 35.71 nm, respectively, and their nanosizes were confirmed by transmission electron microscopy images. Thereafter, 51.30% and 51.02% of the loaded extract was released from F12 and F36 through an artificial cellulose membrane, scavenging 29.89% and 30.05% of DPPH radical activity, respectively. CONCLUSION: The P. urinaria extract was successfully incorporated into a PKOEs-based nanoemulsion delivery system. In vitro release of the extract from the formulations showed DPPH radical scavenging activity. These formulations can neutralize reactive oxygen species and counteract oxidative injury induced by ultraviolet radiation and thereby ameliorate skin aging.
Assuntos
Portadores de Fármacos/química , Phyllanthus/química , Extratos Vegetais/química , Óleos de Plantas/química , Envelhecimento da Pele/efeitos dos fármacos , Administração Tópica , Compostos de Bifenilo , Emulsões/química , Ésteres/química , Etanol/química , Humanos , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Membranas Artificiais , Microscopia Eletrônica de Transmissão , Peso Molecular , Nanopartículas/química , Óleo de Palmeira , Tamanho da Partícula , Permeabilidade , Picratos , Reologia , Absorção CutâneaRESUMO
BACKGROUND: The purpose of this study was to select appropriate surfactants or blends of surfactants to study the ternary phase diagram behavior of newly introduced palm kernel oil esters. METHODS: Nonionic surfactant blends of Tween(®) and Tween(®)/Span(®) series were screened based on their solubilization capacity with water for palm kernel oil esters. Tween(®) 80 and five blends of Tween(®) 80/Span(®) 80 and Tween(®) 80/Span(®) 85 in the hydrophilic-lipophilic balance (HLB) value range of 10.7-14.0 were selected to study the phase diagram behavior of palm kernel oil esters using the water titration method at room temperature. RESULTS: High solubilization capacity was obtained by Tween(®) 80 compared with other surfactants of Tween(®) series. High HLB blends of Tween(®) 80/Span(®) 85 and Tween(®) 80/Span(®) 80 at HLB 13.7 and 13.9, respectively, have better solubilization capacity compared with the lower HLB values of Tween(®) 80/Span(®) 80. All the selected blends of surfactants were formed as water-in-oil microemulsions, and other dispersion systems varied in size and geometrical layout in the triangles. The high solubilization capacity and larger areas of the water-in-oil microemulsion systems were due to the structural similarity between the lipophilic tail of Tween(®) 80 and the oleyl group of the palm kernel oil esters. CONCLUSION: This study suggests that the phase diagram behavior of palm kernel oil esters, water, and nonionic surfactants is not only affected by the HLB value, but also by the structural similarity between palm kernel oil esters and the surfactant used. The information gathered in this study is useful for researchers and manufacturers interested in using palm kernel oil esters in pharmaceutical and cosmetic preparation. The use of palm kernel oil esters can improve drug delivery and reduce the cost of cosmetics.
Assuntos
Hexoses/química , Óleos de Plantas/química , Polissorbatos/química , Tensoativos/química , Emulsões , Ésteres , Interações Hidrofóbicas e Hidrofílicas , Óleo de Palmeira , Transição de Fase , SolubilidadeRESUMO
Aerosol is a new dosage form for wound dressing and wound healing. Concentrate of aerosols which were prepared for wound dressing and wound healing will produced films after sprayed onto the surface of wounds. The aim of this study is to evaluate the mechanical and water vapour permeability properties of the films from the aerosol concentrates. Film forming dispersions contained Haruan extract and Fusidic acid as the active ingredients, hydroxypropyl methylcellulose (HPMC) as polymer and polyethylene glycol (PEG) 400, glycerin and propylene glycol as plasticizers. Haruan extract is used to promote healing and Fusidic acid is added in formula as antibiotic to prevent the infections. The films were prepared by using casting technique. Based on the results, it is concluded that films produced from Formula E1, E2 and F4 possessed good elongation at break but low tensile strength. All Formula E, Formula F4 and F5 were permeable but Formula F5 was brittle and would peel off by themselves from the Petri dish.