Nanosponge-based hydrogel preparation of fluconazole for improved topical delivery

Purpose: To develop polymeric nanosponge based hydrogel system of fluconazole (FZ) for improved delivery for topical application.Method: Six different nanosponge preparations of fluconazole were formulated by oil-in-water (o/w) emulsion solvent diffusion method using various drug to polymer (ethylcellulose, EC) ratios. Polyvinyl alcohol (PVA) and dichloromethane were used to prepare the aqueous and dispersed phases, respectively. The nanosponges (NS) were studied for entrapment efficiency, particle size, structural properties, size and appearance, and in vitro drug release. Furthermore, the hydrogel formulation was evaluated for ex vivo permeation characteristics.Results: Morphological studies revealed porous nanosized particles with the outer surface resembling orange peel. The nanosponges had particle size in the range of 220.2 ± 4.5 to 624.1 ± 10.4 nm. Release studies showed 43.9 ± 3.2 % drug release at 6 h, confirming the sustained release pattern of the drug-loaded nanosponges. Powder x-ray diffraction (PXRD) and Fourier transform infra-red (FTIR) analyses indicate complex formation in the nanosponge structure. Out of six nanosponge formulations prepared, F3 containing FZ and EC in the ratio of 1:0.7 showed optimum physicochemical and release characteristics and, therefore, was selected for hydrogel formulation. Kinetic analysis of the permeation data revealed a Higuchi diffusion pattern. Ex vivo permeation studies indicate that the hydrogel preparation displayed adequate drug permeation through rat abdominal skin.Conclusion: A nanosponge-loaded hydrogel of fluconazole for improved permeation of the drug through skin has been successfully developed. Safety and toxicity tests are required to ascertain its potential suitability for use in humans.Keywords: Fluconazole, Nanosponges, Ethylcellulose, Drug release, Franz diffusion cell, Higuchi diffusio

Quantification of carbon dioxide released from effervescent granules as a predictor of formulation quality using modified Chittick apparatus

Purpose: To develop a method for the measurement of carbon dioxide (CO2) released from effervescent formulations. Methods: Effervescent granules were prepared using sodium bicarbonate and citric acid by fusion and solvent-assisted granulation methods. The amount of CO2 released was determined from the maximum pressure of gas release, time profile of pressure gradient using modified Chittick apparatus and gravimetric changes following effervescence. Results: The amount of CO2 released from effervescent granules prepared by fusion method was 8.125, 8.763 and 7.98 mM/g measured by ideal gas equation, pressure gradient and gravimetric method, respectively. The formulation prepared by solvent-assisted granulation showed 5.525, 5.475 5.36 mM/g of carbon dioxide measured by the above three methods, respectively. The effervescent granules prepared by fusion method showed approximately 2 % loss in effervescence. However, approximately 39 % loss in effervescence was observed for the formulation prepared by solventassisted granulation. The commercial products showed a loss in effervescence in the range of 5 - 15%. Conclusion: Modified Chittick’s apparatus is a useful analytical tool for monitoring of the CO2 from effervescent granules as a function of method of preparation

Development and evaluation of scaffold-based nanosponge formulation for controlled drug delivery of naproxen and ibuprofen

Purpose: To develop and evaluate nanosponge (NS) based sustained release formulations of naproxen (NAP) and ibuprofen (IBU).Method: Six formulations of each candidate drug were prepared by emulsion solvent diffusion method, using varying ratios of polymers, i.e., ethyl cellulose and polyvinyl alcohol. The prepared formulations were evaluated for various parameters including production yield, particle size, polydispersity index, actual drug content and entrapment efficiency. Morphological, structural and thermo-analytical evaluations were performed using various techniques. In vitro release studies were performed on selected formulations.Results: Nanosponge (NS) formulations of naproxen and ibuprofen were successfully prepared by emulsion solvent diffusion method. The particle size of naproxen and ibuprofen nanosponge formulations ranged from 347.6 to 1358 nm and 248.7 to 327.6 nm, respectively. Formulations with equal proportion of ethyl cellulose and drug resulted in nanosponges with the desired particle size. Production yield, actual drug content and entrapment efficiency was dependent on the ratio of ethyl cellulose and polyvinyl alcohol. Formulations with equal proportion showed least PDI values (0.09 for NAP and 0.07 for IBU) and highest zeta potential (-27.2 mV for NAP and -28.2 mV for IBU). Morphological, structural and thermo-analytical analysis confirmed the encapsulation of drugs in nanosponge cavities, and exhibited spherical and porous morphology. Nanosponge formulations gave a sustained release pattern, based on Higuchi model. Drug release mechanism was Fickian followed Korsmeyer-Peppas model, due probably to the porosity of the nanosponge.Conclusion: Sustained release nanosponge formulations of naproxen and ibuprofen have successfully been prepared.Keywords: Nanosponge, Naproxen, Ibuprofen, Emulsion solvent diffusion method, Sustained releas

The Impact Of Nasheman on Capacıty Buıldıng of Hearıng Impaıred (HI) Students

Purpose: The main objective of the study was to explore the impact of Nasheman on the capacity building of hearing- impaired (HI) students. The present study was descriptive and qualitative in nature. Methodology: The population of the study consisted of all the forty eight graduates of Nasheman who have completed their course of skills development from Nasheman. The sample of the study consisted of 14 students, which were selected through a convenient sampling technique. An in-depth interview schedule was used to collect data from selected respondents. Researcher personally visited the selected respondents and interviewed them. Thematic analysis technique was used for data analysis. Findings: The findings of the study revealed that most of the graduates were successful and living honorable lives. The administrative staff was very welcoming and caring. On the other hand, the teaching staff was professionally qualified and hard working.  Implications: More institutes like Nasheman should be established all around the country to facilitate special persons to increase and improve their capacities and there should be more diploma courses offered to facilitate a large number of special persons

PREVELANCE OF METFORMIN-INDUCED GASTROINTESTINAL PROBLEMS

Metformin is used as an anti-diabetic drug among oral hypoglycemic drugs, which produces many gastrointestinal problems. Study aims to investigate the effect of metformin induced gastrointestinal problems and its prevalence. A cross-sectional study design was adapted using convenience sampling technique, at different Diabetic Centers of Lahore and Faisalabad, Pakistan from, June-2017 to November-2017. A total of 300 male and female patients participated in the study between 26 to 85 years and diagnosed with type-II diabetes. Data was directly collected from the patients and prevalence of metformin-induced gastrointestinal intolerance was determined by the symptoms of the patients. Data was analyzed by SPSS version 21. Results showed a significant difference between gender and symptoms (p=0.029). Moreover, the gastrointestinal problems were found to be dose related. A significant difference existed between patients who were taking 500mg and those taking 850 mg of metformin (p=0.006), patients who were taking 500mg and those taking 1000mg of metformin (p=0.000) and patients who were taking 850mg with those taking 1000mg of metformin (p=0.022). The prevelance of metformin-induced gastrointestinal symptoms was 45.8%. Most commonly occurring symptoms were, constipation (41.35%) followed by dyspepsia (27.89%), abdominal pain (26.92%), bloating and heart burn (25%), indigestion (15.38%), anorexia (11.54%), diarrhea (6.58%), flatulence (7.69%), nausea (6.73%) and vomiting (2.88%). It was concluded that gastrointestinal intolerance was more in females as compared to males. The gastrointestinal problems increased with the increase in dose. The side effects occurred were irrespective of the age and the most common gastrointestinal symptom was found to be constipation

Effect of Methanolic Extract of Dandelion Roots on Cancer Cell Lines and AMP-Activated Protein Kinase Pathway

Ethnomedicinal knowledge of plant-derived bioactives could help us in discovering new therapeutic compounds of great potential. Certainly, dandelion has been used in traditional ethno-medicinal systems (i.e., Chinese, Arabian, Indian, and Native American) to treat different types of cancer. Though, dandelion is highly vigorous, but the potential mode of action is still unclear. In the current study, the antiproliferative activity of methanolic extracts of dandelion root (MEDr) on cell viability of HepG2, MCF7, HCT116, and normal Hs27 was investigated. It was observed that MEDr (500 μg/mL) drastically decreased the growth of HepG2 cell line, while the effect on MCF7 and HCT116 cell lines was less pronounced and no effect has been observed in Hs27 cell lines. The MEDr also enhanced the phosphorylation level of AMPK of HepG2 cells, which considered crucial in cancer treatment and other metabolic diseases. The AMPK activation by MEDr noticed in the current study has never been reported previously. The results regarding the number of apoptotic cells (HepG2 cells) were in line with the cell viability test. The current observations clearly demonstrated the potency of MEDr against liver cancer with validation that dandelion could control AMPK and thus cancer in the treated cell lines