Formulation, characterization and optimization of palm oil esters based nano-scaled emulsions for topical delivery of ibuprofen and the evaluation of their anti-inflammatory and analgesic effects.

tujuan utama kajian ini adalah untuk formulasi ibuprofen sebagai suatu emulsi berskala nano baru, yang terdiri daripada ester minyak sawit tersintesis baru sebagai fasa minyak. The main aim of this study stands on formulating ibuprofen as a novel nano-scaled emulsion encompassing newly synthesized palm oil esters as the oil phase

Carbopol 934, 940 and Ultrez 10 as viscosity modifiers of palm olein esters based nano-scaled emulsion containing ibuprofen

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

HPLC and anti-inflammatory studies of the flavonoid rich chloroform extract fraction of Orthosiphon stamineus leaves.

The aim of the present study was to verify the anti-inflammatory activity of Orthosiphon stamineus leaf extracts and to identify the active compound(s) contributing to its anti-inflammatory activity using a developed HPLC method. Active chloroform extract of O. stamineus was fractionated into three fractions using a dry flash column chromatography method. These three fractions were investigated for anti-peritoneal capillary permeability, in vitro nitric oxide scavenging activity, anti-inflammatory and nitric oxide (NO) inhibition using carrageenan-induced hind paw edema method. The flavonoid rich chloroform extract fraction (CF2) [containing sinensetin (2.86% w/w), eupatorin (5.05% w/w) and 3'-hydroxy-5,6,7,4'-tetramethoxyflavone (1.101% w/w)], significantly reduced rat hind paw edema, NO and decreased dye leakage to peritoneal cavity at p < 0.05. IC50 of in vitro NO scavenging of CF2 was 0.3 mg/mL. These results suggest that the anti-inflammatory properties of these CF2 may possibly be due to the presence of flavonoid compounds capable of affecting the NO pathway

Formulation and characterization of palm oil esters based nano-cream for topical delivery of piroxicam

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. Piroxicam is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic activity. It has low solubility in water as well as in oil with Log P value of 1.8. Generally, drugs with Log P value of more than 0.5 are needed to be formulated into a modified dosage form. One of these formulations is nano sized cream. Hence, the ability of formulating of these tricky drugs into dispersed system is questionable. The aim of this study is to investigate the ability of palm oil esters to be the oil phase for formulation of piroxicam into O/W nano-cream. Three points were selected from prepared pseudoternary diagram of palm oil esters and different Tween and Span mixtures. Piroxicam solubility and partition coefficient in oil and external phase was detected. Rheological properties, droplet size, structural properties and zeta potential of the dispersion system containing piroxicam were measured. O/W cream was formed with droplet size measurement by TEM of less than 100 nm. It could be concluded that palm oil esters is suitable oil for the formulation of suitable nano-cream containing piroxicam.Keywords: Palm oil esters; Piroxicam Solubility; partition coefficient; Rheology; Surface activity

Stability studies of nano-cream containing piroxicam

The aim of this study is to study the stability of the nano-cream formula containing the newly synthesized palm oil esters when stored for reasonable storage duration. The prepared 0.5% piroxicam nano-cream formula contained phosphate buffer as external phase, palm oil esters as the oil phase and a combination of (80:20) of Tween 80 and Span 20 as emulsifier at a ratio of 37:25:38, respectively. Piroxicam is a hydro-lipophobic drug. Stability on storage is an important aspect which ensures the dosage form can exert the effects it is supposed to exert for the duration of storage. Droplets size, electrical conductivity, drug content, pH and rheological parameters are the parameters that have been assessed under different temperature to evaluate the stability of nano-cream preparation. Thus, experiments which measure the above parameters were conducted at storage temperatures of 4, 25 and 40οC.The data obtained from the stability study conducted on nano-cream formula showed that this formulation was stable for the whole 3 months period of the study when stored at tested several temperatures.Keywords: Palm oil esters; Nonionic surfactant; Piroxicam; Nano-crea

Stability studies of nano-cream containing piroxicam

The aim of this study is to study the stability of the nano-cream formula containing the newly synthesized palm oil esters when stored for reasonable storage duration. The prepared 0.5% piroxicam nano-cream formula contained phosphate buffer as external phase, palm oil esters as the oil phase and a combination of (80:20) of Tween 80 and Span 20 as emulsifier at a ratio of 37:25:38, respectively. Piroxicam is a hydro-lipophobic drug. Stability on storage is an important aspect which ensures the dosage form can exert the effects it is supposed to exert for the duration of storage. Droplets size, electrical conductivity, drug content, pH and rheological parameters are the parameters that have been assessed under different temperature to evaluate the stability of nano-cream preparation. Thus, experiments which measure the above parameters were conducted at storage temperatures of 4, 25 and 40οC.The data obtained from the stability study conducted on nano-cream formula showed that this formulation was stable for the whole 3 months period of the study when stored at tested several temperatures.Keywords: Palm oil esters; Nonionic surfactant; Piroxicam; Nano-crea

Development of a Stepping Force Analgesic Meter for a Rat Arthritic Model

Behavioural assessment of experimental pain is an essential method for analysing and measuring pain levels. Rodent models, which are widely used in behavioural tests, are often subject to external forces and stressful manipulations that cause variability of the parameters measured during the experiment. Therefore, these parameters may be inappropriate as indicators of pain. In this article, a stepping-force analgesimeter was designed to investigate the variations in the stepping force of rats in response to pain induction. The proposed apparatus incorporates new features, namely an infrared charge-coupled device (CCD) camera and a data acquisition system. The camera was able to capture the locomotion of the rats and synchronise the stepping force concurrently so that each step could be identified. Inter-day and intra-day precision and accuracy of each channel (there were a total of eight channels in the analgesimeter and each channel was connected to one load cell and one amplifier) were studied using different standard load weights. The validation studies for each channel also showed convincing results whereby intra-day and inter-day precision were less than 1% and accuracy was 99.36–100.36%. Consequently, an in vivo test was carried out using 16 rats (eight females and eight males). The rats were allowed to randomly walk across the sensor tunnel (the area that contained eight channels) and the stepping force and locomotion were recorded. A non-expert, but from a related research domain, was asked to differentiate the peaks of the front and hind paw, respectively. The results showed that of the total movement generated by the rats, 50.27 ± 3.90% in the case of the male rats and 62.20 ± 6.12% in that of the female rats had more than two peaks, a finding which does not substantiate the assumptions made in previous studies. This study also showed that there was a need to use the video display frame to distinguish between the front and hind paws in the case of 48.80 ± 4.01% of the male rats and 66.76 ± 5.35% of the female rats. Evidently the assumption held by current researchers regarding stepping force measurement is not realistic in terms of application, and as this study has shown, the use of a video display frame is essential for the identification of the front and hind paws through the peak signals

Global Incidence and Risk Factors Associated With Postoperative Urinary Retention Following Elective Inguinal Hernia Repair

Importance Postoperative urinary retention (POUR) is a well-recognized complication of inguinal hernia repair (IHR). A variable incidence of POUR has previously been reported in this context, and contradictory evidence surrounds potential risk factors.Objective To ascertain the incidence of, explore risk factors for, and determine the health service outcomes of POUR following elective IHR.Design, Setting, and Participants The Retention of Urine After Inguinal Hernia Elective Repair (RETAINER I) study, an international, prospective cohort study, recruited participants between March 1 and October 31, 2021. This study was conducted across 209 centers in 32 countries in a consecutive sample of adult patients undergoing elective IHR.Exposure Open or minimally invasive IHR by any surgical technique, under local, neuraxial regional, or general anesthesia.Main Outcomes and Measures The primary outcome was the incidence of POUR following elective IHR. Secondary outcomes were perioperative risk factors, management, clinical consequences, and health service outcomes of POUR. A preoperative International Prostate Symptom Score was measured in male patients.Results In total, 4151 patients (3882 male and 269 female; median [IQR] age, 56 [43-68] years) were studied. Inguinal hernia repair was commenced via an open surgical approach in 82.2% of patients (n = 3414) and minimally invasive surgery in 17.8% (n = 737). The primary form of anesthesia was general in 40.9% of patients (n = 1696), neuraxial regional in 45.8% (n = 1902), and local in 10.7% (n = 446). Postoperative urinary retention occurred in 5.8% of male patients (n = 224), 2.97% of female patients (n = 8), and 9.5% (119 of 1252) of male patients aged 65 years or older. Risk factors for POUR after adjusted analyses included increasing age, anticholinergic medication, history of urinary retention, constipation, out-of-hours surgery, involvement of urinary bladder within the hernia, temporary intraoperative urethral catheterization, and increasing operative duration. Postoperative urinary retention was the primary reason for 27.8% of unplanned day-case surgery admissions (n = 74) and 51.8% of 30-day readmissions (n = 72).Conclusions The findings of this cohort study suggest that 1 in 17 male patients, 1 in 11 male patients aged 65 years or older, and 1 in 34 female patients may develop POUR following IHR. These findings could inform preoperative patient counseling. In addition, awareness of modifiable risk factors may help to identify patients at increased risk of POUR who may benefit from perioperative risk mitigation strategies