Design and evaluation of molecular organogel based on folic acid as a potential green drug carrier for oral route.

OBJECTIVE: The low molecular weight organogels are interesting carriers for pharmaceutical compounds. However, their uses are limited due to the toxicity burden of the organic solvent used. Hence, this study aimed to prepare organogel using folic acid (FA) in different concentrations as a gelator for propylene glycol (PG) biocompatible solvent. METHODS: The simple mixing method followed by incubation in a water bath at 90 °C was used to prepare organogels. Then, formulations were assessed using different methods including differential scanning calorimetry (DSC), dropping method, attenuated total reflectance - Fourier transform infrared spectroscopy (ATR-FTIR), oscillatory rheology studies, scanning electron microscopy (SEM), and in vitro dissolution study. RESULTS: Gel formation and its consistency were highly depending on FA concentration. The results showed that increasing the concentration of FA in the organogel led to accelerating the gelation process, and the least amount of FA that could gel the PG was 0.25% w/w. However, higher concentrations were needed to create an organogel with excellent properties. The DSC and dropping studies revealed stable organogels formulations at body temperature. The ATR-FTIR showed interactions between the pteridine ring of FA and PG. The strain amplitude and frequency sweep tests demonstrated an increase in storage modulus values as the concentration of FA increased at 37 °C, which were frequency independent at high frequencies. In addition, the SEM exposed the fabrics like the structure of these organogels. Furthermore, the in vitro dissolution of organogel was pH-dependent, with a high possibility of taking place in the large intestine. CONCLUSION: FA/PG organogel formulation is a promising carrier for drug and nutraceuticals compound for the oral delivery system.

Cognitive perspective of osteoporosis among adults with type 2 diabetes mellitus: The Malaysian case.

INTRODUCTION: Osteoporosis and diabetes are highly prevalent diseases. In addition, there is increasing evidence that diabetes is a common risk factor for decreasing bone mineral density and developing osteoporosis and fractures. Data on bone abnormalities in T2DM patients appear to be contradictory and complex, and the exact underlying mechanism is still unclear. Hence, the aims of this study were to assess cognitive perspective of osteoporosis among type 2 diabetes mellitus. METHODS: An observational, cross-sectional study design was chosen, where data were collected using a self-report structured questionnaire including osteoporosis self-efficacy (OSES-M), knowledge Malay version. Quantitative ultrasound was used as prescreening tool for measuring bone health by applying T-score. RESULTS: The results showed that about 231 (51.30%) were males. The average age of the DM patients was 62.67 ± 9.24 years. Moreover, the majority of T2DM patient (343, 76.20%) had poor glycaemic control. The mean ± SD OSES-M total score, OSES-M Exercise subscale and OSES-M Calcium subscale were 731.26 ± 209.83, 357.55 ± 121.23 and 373.71 ± 118.91, respectively. Overall, participants expressed a low self-efficacy for both exercise and calcium intake experiences. In addition, a significant and positive correlation was found between OSES-M and OKT-M total scores (n = 450, rs  = 0.471, p < .05). Also, there were significant correlations between OKT-M subscales and OSES-M subscales. Furthermore, significant and positive correlations were found between T-scores and OSES-M total score (r = .191), OSES-M Exercise subscale (r = .209) and OSES-M Calcium subscale (r = .124). Moreover, significant associations, differences and correlations were found out between OSES-M with many demographic and clinical data. CONCLUSION: Overall, participants expressed a low self-efficacy for both exercise and calcium intake experiences. In addition, only 28.70% of the study population was found to have high OSES-M level. Thus, self-efficacy is important and effective determinants for gaining positive health behaviours towards osteoporosis.

Validation and Assessment of Osteoporosis Self-Efficacy Among Iraqi General Population.

BACKGROUND: Poor quality of life, fractures and disability are the consequences of preventable osteoporosis. OBJECTIVES: The aims of this study were to validate and assess Osteoporosis Self-efficacy Scale (OSES-A) Arabic version among Iraqi general population. METHODS: A cross-sectional study with a random cluster sampling method from the community was used. Forward-backward-forward translation method was used to translate the questionnaire from English to Arabic. Beside OSES-A, Osteoporosis Knowledge Tool (OKT) and Osteoporosis Health Belief Scale (OHBS) Arabic versions were used to assess osteoporosis preventive behaviours. RESULTS: The results showed good face validity and reliability. The construct validity showed two factors which explain 80.86% of the variance. In addition, the result showed low self-efficacy score (658.43±222.014) with 83.33% were found to have low OSES-A level. There were significant associations between age, gender, and self-reported osteoporosis with OSES-A levels. In addition, there were significant differences between age, gender, marital status, family history of osteoporosis, self-reported osteoporosis and osteoporosis diagnosis or screening in relation to total OSES-A scores. Moreover, there were positive correlations between the OSES-A total score with total knowledge and health belief. Multivariate analysis revealed that OKT levels, OHBS levels, age and gender were predictors for OSES-A levels. CONCLUSION: This study showed good cultural adaptation and psychometric properties of OSES-A tool and could be used in any osteoprotective educational program.

The Prevalence of Osteopenia and Osteoporosis Among Malaysian Type 2 Diabetic Patients Using Quantitative Ultrasound Densitometer.

BACKGROUND: Type 2 Diabetes Mellitus (T2DM) and osteoporosis are both chronic conditions and the relationship between them is complex. OBJECTIVE: The aims of this study were to assess the prevalence of Low Bone Mineral density (LBMD, i.e., osteopenia and osteoporosis), as well as, the difference and associations between Quantitative Ultrasound Scan (QUS) parameters with socio-demographic data and clinical related data among T2DM in Penang, Malaysia. METHOD: An observational, cross-sectional study with a convenient sample of 450 T2DM patients were recruited from the outpatient diabetes clinic at Hospital Pulau Pinang (HPP) to measure Bone Mineral Density (BMD) at the heel bone using QUS. In addition, a self-reported structured questionnaire about the socio-demographic data and osteoporosis risk factors were collected. Moreover, the study included the retrospective collection of clinical data from patients' medical records. RESULTS: The mean value of T-score for normal BMD, osteopenic and osteoporotic patients' were (-0.41±0.44), (-1.65±0.39) and (-2.76±0.27), respectively. According to QUS measurements, more than three quarters of T2DM patients (82%) were at high risk of abnormal BMD. The results showed that QUS scores were significantly associated with age, gender, menopausal duration, educational level and diabetic related data. Moreover, the QUS parameters and T-scores demonstrated significant negative correlation with age, menopausal duration, diabetic duration and glycaemic control, as well as, a positive correlation with body mass index and waist to hip ratio. The current study revealed that none of the cardiovascular disease risk factors appear to influence the prevalence of low BMD among T2DM Malaysian patients. CONCLUSION: The study findings revealed that the assessment of T2DM patients' bone health and related factor are essential and future educational programs are crucial to improve osteoporosis management.

Psychometric properties and assessment of the Osteoporosis Health Belief Scale among the general Arabic population.

BACKGROUND: Any educational program should be implemented with a good understanding of the population's beliefs. Therefore, the aims of this study were to validate the Arabic version of the Osteoporosis Health Belief Scale (OHBS-A) and assess the osteoprotective attitude among the Iraqi population. METHODS: A cross-sectional design, with a random cluster sampling method from the community, was used. The forward-backward-forward translation method was used to translate the questionnaire from English to Arabic. In addition, the Arabic version of Osteoporosis Knowledge Tool (OKT-A) and the Arabic version of Osteoporosis Self-Efficacy Scale (OSES-A) were used to assess the osteoprotective behaviors. RESULTS: The results showed good face validity and reliability. The construct validity analysis showed seven factors that explain 72.82% of the variance. In addition, the results revealed a low health belief score (149.95±35.936) with only 36.67% of the study population found to have a high OHBS-A level. The results showed significant differences among employment status, marital status, and osteoporosis (OP) awareness groups in relation to total OHBS-A scores. In addition, there were significant associations between age groups and OP awareness with health belief levels. Moreover, both exercise and calcium intake subscales of the Osteoporosis Knowledge Tool (OKT) positively correlated with all OHBS-A subscales. Exercise and calcium intake subscales of Osteoporosis Self-Efficacy Scale (OSES) positively correlated with the perceived susceptibility and perceived barriers toward exercise and calcium intake. The binary logistic regression analysis showed that OKT levels, OSES levels, and age were predictors of OHBS-A levels. CONCLUSION: Besides cultural obstacles, an educational program for both genders and all age groups is important and should be tailored according to culture needs.

Psychometric properties of Osteoporosis Knowledge Tool and self-management behaviours among Malaysian type 2 diabetic patients.

Osteoporosis is a major growing public health problem and it is clear that much needs to be done to bridge the gap between patients and practitioners. However, the educator must have a valid and reliable tool to evaluate the effectiveness of the teaching and learning that are done. Osteoporosis Knowledge Tool (OKT) provides an important strategy for healthcare professionals to start early intervention for patients who are at risk of osteoporosis. The aims of this study were to translate and examine the psychometric properties of the Malaysian version of the Osteoporosis Knowledge Tool (OKT-M) among 250 type 2 diabetes patients and to assess factors that affect diabetic patients' osteoporosis knowledge. The OKT English version was translated and validated using the internationally accepted and recommended methodology. The sensitivity and specificity of OKT-M was calculated using receiver operating characteristic curve analysis. The face and content validity showed acceptable results. Internal consistency, test-retest reliability, mean difficulty factor and discriminatory power values were 0.72, 0.83, 0.47 ± 0.16 and 0.96, respectively. The cut-off point of the OKT-M to predict osteoporosis/osteopenia was 14 with optimal sensitivity (84.1%) and specificity (85.5%). Regression analysis revealed that health belief, self-efficacy and some demographic data had an impact on the OKT-M. The findings of this validation study indicate that the OKT-M is a reliable and valid tool with good psychometric properties in the Malaysian setting. The OKT-M is an appropriate tool for application in clinical setting to identify patients need for a bone health-promoting intervention regarding lifestyle behaviour changes.

Osteoporosis and type 2 diabetes mellitus: what do we know, and what we can do?

Diabetes mellitus (DM) is a pandemic and chronic metabolic disorder with substantial morbidity and mortality. In addition, osteoporosis (OP) is a silent disease with a harmful impact on morbidity and mortality. Therefore, this systematic review focuses on the relationship between OP and type 2 diabetes mellitus (T2DM). Systematic reviews of full-length articles published in English from January 1950 to October 2010 were identified in PubMed and other available electronic databases on the Universiti Sains Malaysia Library Database. The following keywords were used for the search: T2DM, OP, bone mass, skeletal. Studies of more than 50 patients with T2DM were included. Forty-seven studies were identified. The majority of articles (26) showed increased bone mineral density (BMD), while 13 articles revealed decreased BMD; moreover, eight articles revealed normal or no difference in bone mass. There were conflicting results concerning the influence of T2DM on BMD in association with gender, glycemic control, and body mass index. However, patients with T2DM display an increased fracture risk despite a higher BMD, which is mainly attributable to the increased risk of falling. As a conclusion, screening, identification, and prevention of potential risk factors for OP in T2DM patients are crucial and important in terms of preserving a good quality of life in diabetic patients and decreasing the risk of fracture. Patients with T2DM may additionally benefit from early visual assessment, regular exercise to improve muscle strength and balance, and specific measures for preventing falls. Patient education about an adequate calcium and vitamin D intake and regular exercise is important for improving muscle strength and balance. Furthermore, adequate glycemic control and the prevention of diabetic complications are the starting point of therapy in diabetic patients.

Solubilization of beclomethasone dipropionate in sterically stabilized phospholipid nanomicelles (SSMs): physicochemical and in vitro evaluations.

BACKGROUND: The local treatment of lung disorders such as asthma and chronic obstructive pulmonary disease via pulmonary drug delivery offers many advantages over oral or intravenous routes of administration. This is because direct deposition of a drug at the diseased site increases local drug concentrations, which improves the pulmonary receptor occupancy and reduces the overall dose required, therefore reducing the side effects that result from high drug doses. From a clinical point of view, although jet nebulizers have been used for aerosol delivery of water-soluble compounds and micronized suspensions, their use with hydrophobic drugs has been inadequate. AIM: To evaluate the feasibility of sterically stabilized phospholipid nanomicelles (SSMs) loaded with beclomethasone dipropionate (BDP) as a carrier for pulmonary delivery. METHODS: 1,2-Distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 5000) polymeric micelles containing BDP (BDP-SSMs) were prepared by the coprecipitation and reconstitution method, and the physicochemical and in vitro characteristics of BDP-SSMs were investigated. RESULTS: BDP-SSMs were successfully prepared with a content uniformity and reproducibility suitable for pulmonary administration. The maximum solubility of BDP in SSMs was approximately 1300 times its actual solubility. The particle size and zeta potential of BDP-SSMs were 19.89 ± 0.67 nm and -28.03 ± 2.05 mV, respectively. The SSMs system slowed down the release of BDP and all of the aerodynamic values of the aerosolized rehydrated BDP-SSMs were not only acceptable but indicated a significant level of deposition in the lungs. CONCLUSION: The SSM system might be an effective way of improving the therapeutic index of nebulized, poorly soluble corticosteroids.

Physician adherence to hypertension treatment guidelines and drug acquisition costs of antihypertensive drugs at the cardiac clinic: a pilot study.

Prescribing pattern surveys are one of the pharmacoepidemiological techniques that provide an unbiased picture of prescribing habits. Prescription surveys permit the identification of suboptimal prescribing patterns for further evaluation. The aims of this study were to determine the prescribing trend, adherence of the prescribers to the guideline, and the impact of drug expenditure on drug utilization at the cardiac clinic of Penang Hospital, Malaysia. This was a cross-sectional study. Demographic data of the patients, diagnoses and the drugs prescribed were recorded. The average drug acquisition costs (ADAC) were calculated for each antihypertensive drug class on a daily and annual basis. Adherence to the guideline was calculated as a percentage of the total number of patients. A total of 313 individuals fulfilled the inclusion criteria. The average age of the study population was 59.30 ± 10.35 years. The mean number of drugs per prescription in the study was 2.09 ± 0.78. There were no significant differences in the demographic data. Antihypertensive drugs were used in monotherapy and polytherapy in 20.8% and 79.2% of the patients, respectively. Adherence to the guideline regarding prescription occurred in 85.30% of the patients. The lowest priced drug class was diuretics and the highest was angiotensin-receptor blockers. In conclusion, the total adherence to the guideline was good; the adherence percentage only slightly decreased with a co-existing comorbidity (such as diabetes mellitus). The use of thiazide diuretics was encouraged because they are well tolerated and inexpensive, and perindopril was still prescribed for diabetic patients since it is relatively cheap (generic drug) and its daily dosage is beneficial.

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations.

BACKGROUND: Inhaled corticosteroids provide unique systems for local treatment of asthma or chronic obstructive pulmonary disease. However, the use of poorly soluble drugs for nebulization has been inadequate, and many patients rely on large doses to achieve optimal control of their disease. Theoretically, nanotechnology with a sustained-release formulation may provide a favorable therapeutic index. The aim of this study was to determine the feasibility of using sterically stabilized phospholipid nanomicelles of budesonide for pulmonary delivery via nebulization. METHODS: PEG(5000)-DSPE polymeric micelles containing budesonide (BUD-SSMs) were prepared by the coprecipitation and reconstitution method, and the physicochemical and pharmacodynamic characteristics of BUD-SSMs were investigated. RESULTS: The optimal concentration of solubilized budesonide at 5 mM PEG(5000)-DSPE was 605.71 ± 6.38 µg/mL, with a single-sized peak population determined by photon correlation spectroscopy and a particle size distribution of 21.51 ± 1.5 nm. The zeta potential of BUD-SSMs was -28.43 ± 1.98 mV. The percent entrapment efficiency, percent yield, and percent drug loading of the lyophilized formulations were 100.13% ± 1.09%, 97.98% ± 1.95%, and 2.01% ± 0.02%, respectively. Budesonide was found to be amorphous by differential scanning calorimetry, and had no chemical interaction with PEGylated polymer according to Fourier transform infrared spectroscopy. Transmission electron microscopic images of BUD-SSMs revealed spherical nanoparticles. BUD-SSMs exhibited prolonged dissolution behavior compared with Pulmicort Respules (P < 0.05). Aerodynamic characteristics indicated significantly higher deposition in the lungs compared with Pulmicort Respules. The mass median aerodynamic, geometric standard deviation, percent emitted dose, and the fine particle fraction were 2.83 ± 0.08 µm, 2.33 ± 0.04 µm, 59.13% ± 0.19%, and 52.31% ± 0.25%, respectively. Intratracheal administration of BUD-SSMs 23 hours before challenge (1 mg/kg) in an asthmatic/chronic obstructive pulmonary disease rat model led to a significant reduction in inflammatory cell counts (76.94 ± 5.11) in bronchoalveolar lavage fluid compared with administration of Pulmicort Respules (25.06 ± 6.91). CONCLUSION: The BUD-SSMs system might be advantageous for asthma or chronic obstructive pulmonary disease and other inflammatory airway diseases.