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Topical preparations have a problem of being wiped off after a short time, which results in low activity of the active moiety. In this research, topical organogels (OGs) were prepared with different oils for the controlled action of miconazole nitrate. Various oils were checked for their gel-forming ability. Controlled release OGs were prepared with a 15% concentration of glyceryl monostearate. Differential scanning calorimetry was performed to study the thermal behavior of gels. X-ray diffraction revealed that the drug was changed into an amorphous form from the crystalline form. The absence of any interaction between the active ingredient and excipients was concluded by Fourier Transform Infrared spectroscopy. Permeability studies were carried out with cellulose acetate membrane by using Franz diffusion cell containing phosphate buffer saline pH 7.4. The release of drug followed the Weibull model. A frequency sweep test was performed to study the rheological behavior of optimized formulations. Rheology revealed the true nature of formulations whether they are gels or just viscous fluids. Images of scanning electron microscopy showed a network formed by the gelator molecules. The antifungal activity was checked against C. albicans and A. niger and it was best by the formulation made by TT. It was concluded that all the OGs gave controlled topical antifungal action.

Here, we developed oral fast disintegrating film (ODF) of ranitidine hydrochloride (RHCl) by solvent casting method and assessed the impact of various formulation ingredients i.e. polymer concentration, type of plasticizers and superdisintegrants. Optimized film was developed with hydroxypropyl methyl cellulose (HPMC E5, 3% w/v) as film matrix, propylene glycol (PG) (10% w/w of polymer) as plasticizer and Pearlitol flash® (PF) (10% w/w of polymer) as release modifier. This film was chosen based on appearance, transparency, thickness, folding endurance and in vitro disintegration time (DT). Later on, optimized film was loaded with drug (50% w/w of polymer) (A12), which disintegrated within 15 seconds and released 81% of RHCl within two minutes. Furthermore, FTIR studies confirmed the absence of drug film ingredients interaction. SEM showed even distribution of RHCl and all excipients. Thus, A12 will be palatable for geriatric patients and helpful to avoid premature intestinal degradation.

Low aqueous solubility and bioavailability is the limiting factor to achieve desired therapeutic efficacy for variety of new and existing drug moieties. The goal of the present study was to explore the effects of β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) on the solubility and dissolution profile of diflunisal (DIF) prepared by using two different methods (physical mixing and solvent evaporation) at DIF-cyclodextrins weight ratios of 1:1, 1:2 and 1:4. The phase solubility studies demonstrated that DIF solubility increased proportionally with an increase in βCD and HPβCD concentration. The inclusion complexes were subjected to characterization of scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Solvent evaporation yielded higher DIF solubility than physical mixing method. HPβCD-DIF inclusion complexes yielded higher dissolution profile than βCD complexes when prepared under same experimental design. FTIR, DSC and XRD confirmed the successful inclusion of DIF into cyclodextrin (βCD/HPβCD) by both preparation methods with enhanced water solubility and drug release in comparison with pure drug.

Although ebastine (EBT) can impede histamine-induced skin allergic reaction and persuade long acting selective H1 receptor antagonistic effects but its poor water solubility circumscribed its clinical application. The main objective of this research work was to improve the aqueous solubility and oral bioavailability of EBT by preparing EBT-loaded bilosomes (EBT-PC-SDC-BS). A thin film hydration method was used to prepare ebastine loaded bilosomes. The prepared-formulations were optimized considering size, morphology and entrapment efficiency. The SEM images revealed regular and spherical shape of bilosomes. Average size of the prepared EBT-PC-SDC-BS was 665.8 nm and zeta potential was around-32.9 mV with 89.05 % average entrapment efficiency (EE).Importantly, the solubility of EBT in water was amplified up to 17.9 μg/ml compared to pure drug (2 μg/mL) reflecting a highest solubility increase of 751 %. In vitro drug release results of prepared EBT-PC-SDC-BS exhibited improved release behavior. Finally, it is established from the results that the EBT-PC-SDC-BS could function as a favorable nano-carrier system to improve the solubility as well as dissolution of EBT.

A stability indicating reverse phase-HPLC method was designed for determination of dexibuprofen in drug solution and in nanocream formulation. Chromatographic conditions were optimized simply by adjusting the content and different compositions of reverse phase associated with mobile phases. Different parameters like specificity, limit of quantification (LOQ), limit of detection, linearity, range, system suitability, precision and accuracy were determined. Stability studies of dexibuprofen in nanocream were taken under the stressed situations of alkali, acid, oxidation process, UV and heat degradation. Tailing factor and % RSD were found >2000 and <2% respectively. The method was identified linear over the range of 0.2-1.6mg/ml having co-efficient of correlation 0.9995. Intra-day and inter- day precision and accuracy values for dexibuprofen were < 0.6% and <1.1032 and < 0.3% and 1.10% respectively. Stability studies showed that dexibuprofen was stable in nanocream against alkali, acid, oxidation, UV light and heat. The developed validated method was precise and accurate for the evaluation of dexibuprofen in solution as well as in nanocream formulation.

Cupric ions are hazardous to human beings and their removal from the body is very necessary. The blends of IRP69H (AMBERLITE IRP-69 [H + ] RESIN), DC20H (DOWEX ™ 20 [H+] Resin), DMSCH (DOWEX™ MARATHON™ MSC [H+] Resin) and Kappa Carrageenan (κ-) were utilized for the removal of ions of Cu 2+ from the blood. They were subjected to docking studies which showed that there is no significant interaction with the blood albumin. IER dose of 0.5 mg/10mL of IRP69H/κ-, DMSCH/κ-, and DC20H/κ- was essential for the 2+ ion removal. At pH 5.4, optimal 2+ ions adsorption efficiency was attained. The adsorption capacities of 2+ were in the order of IRP69H/κ->DC20H/κ->DMSCH/κ-. While the data fitted well to Freundlich, Langmuir and Dubinin-Radushkevich. Pseudo-second order was followed for 2+ adsorption for DMSCH/κ- and DC20H/κ- while the pseudo-first order was demonstrated well for IRP69H/κ-.

The present study was designed to develop novel lipid microparticles in order to improve solubility, dissolution and bioavailability of a lipophilic drug of BCS class II, lamotrigine. For that purpose, increase in solubility of the model drug was investigated using different lipids and the promising lipids were further used for the fabrication of microparticles. Solid lipid (GMS) and liquid lipid (olive oil) were used along with an emulsifier (Tween 80) and a stabilizer (Poloxamer 188) to prepare mircoparticles by melt emulsification method. Prepared formulations were characterized for physicochemical properties such as solubility, particle size, zeta potential, polydispersity index and entrapment efficiency. In vitro dissolution studies were carried out in 0.01 N HCl for 24 h. The findings provided that the solubility of lamotrigine was reasonably increased in GMS, olive oil, Tween 80 and poloxamer 180. The lamotrigine solubility was increased 4.92 fold with G4 microparticles formulation. Size analysis revealed that the microparticles were in range of 11.1 to 178.8 μm and the zeta potential values were from -13 to -20 mV. Microparticles prepared with solid and liquid lipids exhibited satisfactory entrapment efficiency ranging from 59 to 87%. Conclusively, the outcomes of the studies suggest the appropriateness of selected ingredients for improving solubility as well as loading of lamotrigine in microparticles for its sustained and effective delivery.

Flurbiprofen, an NSAID, is a water insoluble drug that is also notorious for gastric irritation and inflammation. This study was aimed at using a natural gastrprotective oil as the internal phase to develop flurbiprofen micro emulsion (ME) to improve it solubility and ameliorate its gastric side effects. Upon screening of ME components for drug solubility, clove oil, tween 80 and transcutol were identified as the oil, surfactant and co surfactant, respectively, with higher flurbiprofen solubility. Pseudo-ternary phase diagrams revealed that the ME made with surfactant only and without co-surfactant displayed the similar ME region as made with the mixture of surfactant and co-surfactant. Furthermore, drug loaded oil was also used to draw pseudo-ternary phase diagram and a very little decrease in the ME region was observed. Therefore, co-surfactant free flurbiprofen loaded ME was developed to avoid side effects associated with the use of excessive surfactant quantities. ME were found to possess size in the range of 11-41 nm with PDI <0.5 and a slightly negative charge. Conductivity, pH and refractive indices of the selected MEs were well in the range. Drug release studies indicated maximum drug release from MEs within 5 min. Analysis of the gastric mucosa of rats after oral administration of drug solution and drug loaded ME confirmed that clove oil based ME provided significant protection against the NSAIDs induced gastric damage.

Medicinal and aromatic plants contribute to major portion of the flora. The plant materials obtained from these plants are used in the pharmaceuticals, cosmetics, and drug industries. Tamarix dioica is locally used in the management of splenic and hepatic inflammation as well as diuretic and carminative. It also possesses cytotoxic, antimicrobial, antifungal and anti-inflammatory activity. The present study investigates the anti-inflammatory, anti-pyretic and analgesic activities of the crude methanolic extract from Tamarix dioica. Anti-inflammatory activity was measured by Carrageenan Induced Paw Edema and Xylene Induced Ear Edema methods. Pyrexia induction with Brewer's yeast assay was used to determine antipyretic activity and analgesic activity was estimated by acetic acid induced writhing and hot plate methods. The data indicated that anti-inflammatory, anti-pyretic and analgesic activities of the crude methanolic extract from Tamarix dioica was dose and time dependent when measured by different assays. Exposure of model animal to increasing concentrations of the plant extract for longer period increased their anti-inflammatory, anti-pyretic and analgesic activities. Significantly highest anti-inflammatory, anti-pyretic and analgesic activities were noted at highest doses of the crude methanolic extract for longer exposure compared with their respective controls.

The present study describes the synthesis of mesoporous silica nanoparticles using a modified sol-gel method. Various proportions of acetonitrile-water mixtures were utilized so as to optimize the reaction mixture for facile synthesis of mesoporous silica nanoparticles with controlled particle size for the very first time. After carefully adjusting the water and acetonitrile contents i.e. to 1:1 v/v ratio, a more uniform and small sized nanoparticles were achieved. The resultant particles were 140 nm in size having pore size of approximately 5.9 nm and were safe to be used in the cellular system, as confirmed by the in vitro cytotoxicity studies.

A simple, specific, sensitive, robust, accurate and precise reverse-phase high performance liquid chromatographic (RP-HPLC) method was developed and validated for simultaneous determination of sofosbuvir (SOF) and velpatasvir (VLP) in fixed dose combination tablets and plasma. Validation parameters, such as system suitability, accuracy, inter-day and intra-day variances, specificity, linearity, limit of detection (LOD), limit of quantification (LOQ), robustness and stability were assessed following the standards set by the International Conference on Harmonization (ICH). The isocratic elution of SOF and VLP was carried out under ambient conditions using ammonium acetate buffer (pH = 7.0), acetonitrile and methanol (20:40:40, v/v/v) as mobile phase flowing through a Promosil C18 column at a flow rate of 1.0 mL/min. The average retention time of SOF and VLP was 3.72 min and 7.09 min, respectively. The LOD and LOQ of SOF were 0.23μg/mL and 2.48μg/mL, respectively; while those of VLP were 0.70μg/mL and 7.52μg/mL, respectively. The regression coefficient (r2) was 0.998. The relative standard deviation (RSD) was less than 2% for precision. The recovery of both the analytes remained within 100±1%. All other validation parameters complied with ICH guidelines. The analytes remained stable throughout the analytical procedure. Moreover, this method was successfully applied to assess the in vitro dissolution of SOF and VLP loaded fixed dose combination tablets. Same method with same mobile phase was applied on rat plasma and there was no interference.

Lovastatin (LSN), a potent anti-hyperlipidemic drug, possesses poor bioavailability due to its very low aqueous solubility. The objective of this study was to establish a relationship between increased drug solubility before reaching site of absorption or increasing drug solubility at target absorption site for accentuated bioavailability of LSN. Composites of LSN with oppositely natured pH-sensitive acrylate polymers, cationic Eudragit EPO (EPO) and anionic Eudragit L100 (L100), were fabricated with physical trituration and kneading methods. Formulations were characterized for solubility, FTIR, PXRD, DSC, SEM, dissolution and bioavailability studies in rats. Interestingly, we observed that physical mixtures of EPO outmatched its kneaded formulations, whereas the physical mixtures and kneaded dispersions of L100 were virtually similar in characteristics. EPO was superior in boosting LSN solubility in the respective medium than the L100. Moreover, EPO produced immediate release profile in gastric environment whereas L100 offered sustained release of LSN in intestinal milieu. Bioavailability studies in rats further supported the EPO formulation in terms of shorter T max , higher C max and heightened AUC.

The present study was designed to investigate the antihyperglycemic effect of Persea duthieion blood glucose concentration and body weight in alloxan induced diabetic hyperglycemic rabbits. The results illustrated significant antihyperglycemic activity of crude extract with 17.44% and 28.02% amelioration at 25 and 50mg/kg p.o. respectively after 24th day of drug treatment; equally supported by body weight recovery. Upon fractionation, most dominant antihyperglycemic effect was displayed by aqueous fraction with 22.12% and 34.43% effect followed by ethyl acetate fraction with 24.32% and 32.05% effect at 25 and 50mg/kg p.o. respectively after 24th day of drug treatment. The effect on blood glucose was also reflected on body weight of animals. In conclusion, our study documented marked antihyperglycemic activity of extract/fractions of P. duthiei.

Manifestation of microbial spoilage of any product by bacteria and to assess the effectiveness of the anti-microbial preservatives (parabens) used for the prevention and stability purpose. The aim of the present work is to study the effectiveness of preservatives used in the antacid suspensions and to analyze the effect of microbial growth on the quality of respective antacid suspensions. Samples of various antacid suspensions were randomly collected from local market and Government hospital pharmacies. Three different antacid formulations were prepared in the laboratory. All the formulations were preliminarily evaluated on the basis of organoleptic characteristics, pH, viscosity and assay. Efficacy of the preservative system in suspension formulation was determined by inoculating the samples in its final container, with specific strains of bacteria i.e. Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 9027 and Staphylococcus aureus ATCC 6538, taking samples from the inoculated preparation at specified intervals of time i.e. 0 time, 07 days, 14 days and 28 days, growing it on nutrient agar medium and colony forming units (CFUs) were scored by plate count. At the same time the samples were also subjected to qualitative and quantitative testing. The decrease in CFU and alteration in assay, pH and viscosity was observed in all the formulations except formulation M2 and F3 that showed stability throughout the study period.

A simple and precise RP-HPLC method was developed for simultaneous determination of piroxicam and ofloxacin in pharmaceutical formulations and human serum. Optimum separations of piroxicam, ofloxacin and stress-induced degradation products were achieved by use of Hypersil BDS C8 column (250 x 4.6mm, 5 μm). The mobile phase was a mixture of acetonitrile: 0.012M K2HPO4: 0.008M sodium citrate (both buffers mixed and pH adjusted to 2.8) (50:25:25 v/v/v) delivered at flow rate of 1.5 mL min⁻¹ using DAD at 254 nm. Response was linear function of concentration over the ranges of 70-130 mg mL⁻¹ for piroxicam and ofloxacin (r² ≥ 0.999). The method efficiently separated the analytical peaks from degradation products with acceptable tailing and resolution. The developed method was successfully used for concurrent analysis of piroxicam and ofloxacin in pharmaceutical formulations, human serum and in vitro drug interaction studies.

The cardiovascular activity of aqueous methanolic extract of Paspalidium flavidum L. was evaluated on isolated rabbit heart and aorta. Heart rates, force of contraction and perfusion pressure were assessed in the presence of different concentrations of extract and adrenaline by using Langendorff's technique. Moreover, the vasoconstriction effects were studied in rabbit aorta using isolated organ bath. The results indicated that the extract (1ng-100 μ g/ml) exhibited a significant increase in heart rate, contractility and perfusion pressure of isolated rabbit's heart; with a maximum effect at 1ng/ml, which was comparable to adrenaline (1 μ g/ml). Similarly, adrenaline at doses from 1-10 μ g/ml produced a significant dose dependant increase in all the cardiac parameters. The cardiotonic effects of the extract were significantly blocked by propranolol (10(-5)M) while an increase in perfusion pressure was completely antagonized by verapamil (10(-6)M). Activity of cardiac marker enzymes was also significantly raised in the perfusate of isolated heart pretreated with the extract. In rabbit aorta, the extract exhibited a dose dependent vasoconstriction effect however it did not increase the tone of aorta when pre-treated with verapamil (10(-6)M). It is conceivable therefore; that the cardiotonic and vasoconstriction effects of the extract might be due to its agonistic actions on β-receptors and Ca(+2) channels.

This paper is based on data recorded from various literatures pertaining to ethnophytomedicinal recipes used against diabetes in South East Asia (India, Pakistan and Srilanka). Traditional plant treatments have been used throughout the world for the therapy of diabetes mellitus. In total 419 useful phytorecipes of 270 plant species belonging to 74 Angiospermic families were collected. From the review it was revealed that plants showing hypoglycemic potential mainly belong to the families, Cucurbitaceae (16 spp.), Euphorbiaceae (15 spp.), Caesalpiniaceae and Papilionaceae (13 spp. each), Moraceae (11 spp.), Acanthaceae (10 spp.), Mimosaceae (09 spp.), Asteraceae, Malvaceae and Poaceae (08 spp. each), Hippocrateaceae, Rutaceae and Zingiberaceae (07 spp. each), Apocynaceae, Asclepiadaceae and Verbenaceae (06 spp. each), Apiaceae, Convolvulaceae, Lamiaceae, Myrtaceae, Solanaceae (05 spp.each). The most active plants are Syzigium cumini (14 recipes), Phyllanthus emblica (09 recipes), Centella asiatica and Momordica charantia (08 recipes each), Azadirachta indica (07 recipes), Aegle marmelos, Catharanthus roseus, Ficus benghalensis, Ficus racemosa, Gymnema sylvestre (06 recipes each), Allium cepa, A. sativum, Andrographis paniculata, Curcuma longa (05 recipes each), Citrullus colocynthis, Justicia adhatoda, Nelumbo nucifera, Tinospora cordifolia, Trigonella foenum-graecum, Ziziphus mauritiana and Wattakaka volubilis (4 recipes each). These traditional recipes include extracts, leaves, powders, flour, seeds, vegetables, fruits and herbal mixtures. Data inventory consists of botanical name, recipe, vernacular name, English name. Some of the plants of the above data with experimentally confirmed antidiabetic properties have also been recorded. More investigations must be carried out to evaluate the mechanism of action of diabetic medicinal plants. Toxicity of these plants should also be explained. Scientific validation of these recipes may help in discovering new drugs from these medicinal plants for diabetes.

To examine the serum antioxidant levels like vit-C, vit-E and glutathione in patients with renal diseases who were subjected to dialysis and to evaluate the antioxidant by FRAP method. To find out the involvement of free radicals in pathogenesis of renal disease. Fifty patients with high levels of creatinine and urea level were included in the study of dialysis. A difference of antioxidant level of vit-C, vit-E and glutathione was observed. The study therefore suggests the importance of assessing these marker oxidative stress antioxidant capacities in renal disease during dialysis.

Lipid profile in cardiac patients (myocardial infarction, angina pectoris, coronary heart disease, ischaemic heart disease), diabetic patients and normal humans was investigated. Total serum cholesterol, high density lipoprotein cholesterol (HDL-C), low density lipoprotein cholesterol (LDL-C), triglycerides, blood glucose, calcium, potassium and sodium were determined, employing established methods and procedures. Higher level of total cholesterol, LDL-C and triglyceride were found in both cardiac and diabetic patients, however, cardiac patients had much lower level of HDL-C as compared to normal humans. Age wise comparison revealed that level of total cholesterol; triglyceride and LDL-C were elevating while the level of HDL-C were decreasing with the age in cardiac and diabetic patients. Sex wise comparison showed that females had higher HDL-C level than males and therefore had fewer incidences of heart diseases. The level of Ca++, K+ and Na+ were similar in all age groups and sexes. No significant elevation in the level of these electrolytes was discovered.