Effect of surfactant and surfactant blends on pseudoternary phase diagram behavior of newly synthesized palm kernel oil esters

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 waterin- 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

Formulation and in vitro release evaluation of newly synthesized palm kernel oil esters-based nanoemulsion delivery system for 30% ethanolic dried extract derived from local Phyllanthus urinaria for skin antiaging

Elrashid Saleh Mahdi1, Azmin Mohd Noor1, Mohamed Hameem Sakeena1, Ghassan Z Abdullah1, Muthanna F Abdulkarim1, Munavvar Abdul Sattar2 1Department of Pharmaceutical Technology, 2Department of Physiology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Pulau Pinang, Malaysia 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. Keywords: nanoemulsions, Phyllanthus urinaria, skin antiaging, palm kernel oil ester

Effect of surfactant and surfactant blends on pseudoternary phase diagram behavior of newly synthesized palm kernel oil esters

Elrashid Saleh Mahdi1, Mohamed HF Sakeena1, Muthanna F Abdulkarim1, Ghassan Z Abdullah1,3, Munavvar Abdul Sattar2, Azmin Mohd Noor11Department of Pharmaceutical Technology, 2Department of Physiology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden, Penang, Malaysia; 3Department of Pharmaceutical Technology, International Medical University, Bukit Jalil, Kuala Lumpur, MalaysiaBackground: 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.Keywords: phase diagram, palm kernel oil esters, nonionic surfactants, microemulsion

Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream

During recent years, there has been growing interest in use of topical vehicle systems to assist in drug permeation through the skin. Drugs of interest are usually those that are problematic when given orally, such as piroxicam, a highly effective anti-inflammatory, anti-pyretic, and analgesic, but with the adverse effect of causing gastrointestinal ulcers. The present study investigated the in vitro and in vivo pharmacodynamic activity of a newly synthesized palm oil esters (POEs)-based nanocream containing piroxicam for topical delivery

Modification and Validation of an HPLC Method for Quantification of Piroxicam

Piroxicam is a NSAID that is widely used in the treatment of joint pain and osteoarthritis. The objectives of the study were to modify and validate HPLC method so as to obtain an accurate, sensitive and precise method to quantify piroxicam concentrations without interference from the other ingredients presence in the formulation. The method published by Owen et al. was adapted and modified to suit the above requirements. The modification was carried out on the mobile phase as the mobile phase used by the authors was not able to separate the drug peak from the interference of the formulation excipients. The modified mobile phase consisted of 5 mM of disodium hydrogen phosphate adjusted to pH 3 with concentrated ortho phosphoric acid, methanol, acetonitrile and glacial acetic acid at ratios of 27:20:52:1 respectively. The method was validated and found to be specific, precise, accurate and reproducible even when run at different times of the same day or on different times on different days. The limit of detection and quantification were determined to be 0.035 μg/ml and 0.0625 μg/ml respectively. It could be concluded that this method could be used to determine piroxicam concentration in the samples collected from in vitro study of permeability through the synthetic membrane and excised rat skin.Keywords: Piroxicam, HPLC, Quantification analysis, Modification

Study of Pseudoternary Phase Diagram Behaviour and the Effect of Several Tweens and Spans on Palm Oil Esters Characteristics

Palm oil esters are high molecular weight esters oil that has been newly synthesized by University Putra Malaysia researchers. It has received a lot of attention for its pharmaceutical and chemical application. The aim of this study is to study the effects of the palm oil esters with different HLB surfactant mixture on the ternary diagrams behaviour and to confine the various systems resulted from these combinations. These systems include traditional emulsion, gel area, transpernat micro-emulsion area, O/W and W/O emulsions. In this study, pseudoternary phase diagrams of water, POEs and non-ionic surfactant mixture of several HLB values were constructed using water titration method. The resultant mixtures collected after each addition and mixing of water were analysed visually, along with conductivity, dilution in water and dye test (methylene blue) to classify them as O/W emulsion (transparent and opaque) or W/O (opaque) and liquid or gel. As a conclusion, palm oil esters were found to be suitable for the formulation of different types of emulsion. Additionally, different HLB value of non-ionic surfactant(s) exhibited different pseudoternary phase diagram characteristics.Keywords: palm oil esters, Tween, Span, Pseudoternary phase diagram, O/W emulsio

Study of Pseudoternary Phase Diagram Behaviour and the Effect of Several Tweens and Spans on Palm Oil Esters Characteristics

Palm oil esters are high molecular weight esters oil that has been newly synthesized by University Putra Malaysia researchers. It has received a lot of attention for its pharmaceutical and chemical application. The aim of this study is to study the effects of the palm oil esters with different HLB surfactant mixture on the ternary diagrams behaviour and to confine the various systems resulted from these combinations. These systems include traditional emulsion, gel area, transpernat micro-emulsion area, O/W and W/O emulsions. In this study, pseudoternary phase diagrams of water, POEs and non-ionic surfactant mixture of several HLB values were constructed using water titration method. The resultant mixtures collected after each addition and mixing of water were analysed visually, along with conductivity, dilution in water and dye test (methylene blue) to classify them as O/W emulsion (transparent and opaque) or W/O (opaque) and liquid or gel. As a conclusion, palm oil esters were found to be suitable for the formulation of different types of emulsion. Additionally, different HLB value of non-ionic surfactant(s) exhibited different pseudoternary phase diagram characteristics.Keywords: palm oil esters, Tween, Span, Pseudoternary phase diagram, O/W emulsio

Stability Studies of Nano-Scaled Emulsions Containing Ibuprofen for Topical Delivery

Biphasic systems, like emulsions and nano-scaled emulsions, are naturally unstable. The extent and rate of the destabilization process differ from system to another. The stability of such systems upon storage is an important aspect to ensure their abilities to exert the expected effects and consequently render them pharmaceutically acceptable. In the present study, the stability of the nano-scaled emulsion containing newly synthesized palm oil esters (POEs) was assessed under different storage conditions and over specified durations. Three nano-scaled emulsion formulae were chosen for this investigation. They basically comprised ibuprofen as the active ingredient, triethanolamine aqueous solution pH 7.4 as the external phase, POEs as the oil phase, Tween 80 as an emulsifier, Carbopol® 940 as the rheology modifier and menthol or limonene as penetration promoters. The evaluation processes were carried out at several temperatures (4, 25 and 40 °C) with factors, such as droplets size, electrical conductivity, drug content, pH and flow properties were relatively held constant. The data collectively showed that all formulations were stable over an observation period of three months.Keywords: Ibuprofen, nano-scaled emulsion, palm oil esters, stabilit

Stability Studies of Nano-Scaled Emulsions Containing Ibuprofen for Topical Delivery

Biphasic systems, like emulsions and nano-scaled emulsions, are naturally unstable. The extent and rate of the destabilization process differ from system to another. The stability of such systems upon storage is an important aspect to ensure their abilities to exert the expected effects and consequently render them pharmaceutically acceptable. In the present study, the stability of the nano-scaled emulsion containing newly synthesized palm oil esters (POEs) was assessed under different storage conditions and over specified durations. Three nano-scaled emulsion formulae were chosen for this investigation. They basically comprised ibuprofen as the active ingredient, triethanolamine aqueous solution pH 7.4 as the external phase, POEs as the oil phase, Tween 80 as an emulsifier, Carbopol® 940 as the rheology modifier and menthol or limonene as penetration promoters. The evaluation processes were carried out at several temperatures (4, 25 and 40 °C) with factors, such as droplets size, electrical conductivity, drug content, pH and flow properties were relatively held constant. The data collectively showed that all formulations were stable over an observation period of three months.Keywords: Ibuprofen, nano-scaled emulsion, palm oil esters, stabilit

Modification and Validation of an HPLC Method for Quantification of Piroxicam

Piroxicam is a NSAID that is widely used in the treatment of joint pain and osteoarthritis. The objectives of the study were to modify and validate HPLC method so as to obtain an accurate, sensitive and precise method to quantify piroxicam concentrations without interference from the other ingredients presence in the formulation. The method published by Owen et al. was adapted and modified to suit the above requirements. The modification was carried out on the mobile phase as the mobile phase used by the authors was not able to separate the drug peak from the interference of the formulation excipients. The modified mobile phase consisted of 5 mM of disodium hydrogen phosphate adjusted to pH 3 with concentrated ortho phosphoric acid, methanol, acetonitrile and glacial acetic acid at ratios of 27:20:52:1 respectively. The method was validated and found to be specific, precise, accurate and reproducible even when run at different times of the same day or on different times on different days. The limit of detection and quantification were determined to be 0.035 μg/ml and 0.0625 μg/ml respectively. It could be concluded that this method could be used to determine piroxicam concentration in the samples collected from in vitro study of permeability through the synthetic membrane and excised rat skin.Keywords: Piroxicam, HPLC, Quantification analysis, Modification