Surfactant and polymers are generally used in the controlled drug delivery systems. Surfactant and polymer systems form supra-assemblies, which are extensively exploited as active delivery vehicles. These systems include liquid crystalline aggregates (e.g., liposomes and cubosomes) or cross-linked gel networks (hydrogels) that load, stabilize, and eventually deliver active ingredients. The potential for utilizing a particular active with a vehicle depends on the physicochemical properties of both. To achieve therapeutic effects, it must be possible to load sufficient amounts of the active, which largely depends on the interaction of the vehicle and active. Further, the integrity of the active must be retained through all stages: preparation, storage, and use. The release rate of actives must be controlled to achieve optimal drug release profiles, while ease of preparation and vehicle stability must also be considered. An optimal delivery vehicle must successfully encompass all these properties.Cubosomes are bicontinuous cubic phase liquid crystals have many properties that make them appealing as a universal vehicle for drug delivery. Luzzati et al. 1) first documented its geometric model supplied later by Scriven.2) Which is in the past decade have been examined for drug delivery.3) The surfactant assembles into bilayers that are twisted into a three dimension, periodic, minimal surface forming tightly packed structure, like "honeycombed" with bicontinuous domains of water and lipid.Cubosome particles are first prepared by mechanical fragmentation of the cubic lipid-water phase in a three-phase region containing a liposomal dispersion and to differentiate from liposomes, these particles have been termed as cubosomes. [4][5][6][7][8] Its structure is different from liposomes because its structure can simultaneously accommodate water-soluble, lipid-soluble, and amphiphilic molecules.Three structure of cubosomes have been proposed by Luzzati et al. 9); (i) Pn3m (D-surface) (Diamond surface), (ii) Ia3d (G-surface) (Gyroid surface), and (iii) Im3m (P-surface) (Primitive surface), in terms of nodal surfaces.The structure generally maintains the efficacy; stability of actives such as vitamins 10) and proteins. 11) Cubosomes are thermodynamically stable; lasting indefinitely.12) Colloidal dispersions of cubosomes can be stabilized by the addition of polymers.13) They also possess the potential for controlled delivery of actives, where diffusion is governed by the tortuous diffusion of the active through the "regular" channel structure of the cubic phase.14) Cubosomes possess a sufficient average degree of molecular orientation order to characterize by structural symmetry, and often form in aqueous surfactant system at relatively high ampiphile concentrations.History Luzzati and Husson 15) and Luzzati et al. first recognized the existence of cubic phases in lipid-water system using X-ray scattering measurement. Fontell et al. 16) drew similar conclusions regarding cubic phase in ternary systems of ampiphiles, oils and ...
Objective: The objective of the present research investigation involves synthesis and biological evaluation of antidiabetic activity of benzothiazole derivatives. Methods:A novel series of benzothiazole derivatives 7(a-l) were synthesised and synthesised compounds were characterised for different physical and chemical properties like molecular formula, molecular weight, melting point, percentage yield, Rf value, IR, 1 HNMR, 13Results: All the synthesised derivatives showed significant biological efficacy. The compound 7d at 350 mg/kg exerted maximum glucose lowering effects whereas 7c showed minimum glucose lowering effects. All the compounds were effective, and experimental results were statistically significant at p<0.01 and p<0.05 level.CNMR and mass spectroscopy. The newly synthesised benzothiazole derivatives were subsequently assayed in vivo to investigate their hypoglycemic activity by the alloxan-induced diabetic model in rats. Conclusion:From the results, it is clear that compound 7d demonstrated potent anti-diabetic activity and would be of better use in drug development to combat the metabolic disorder in future.
Benign prostate hyperplasia (BPH) is common among above 50 years age group, interfere with normal activities of lower urinary tract function and reduce the sense of well being. It can also be progressive, with a lost of urinary retention, bladder infection, bladder calculus and renal failure. Although many men with mild to moderate symptoms to well without therapy, others have gradually increasing symptoms and require medical therapy or surgery. BPH is the non-malignant, uncontrolled growth of cells in the prostate gland. This cell growth usually occurs in the tissue that surrounds the urethra as it passes through the prostate gland to the bladder. As BPH progresses, the gland constricts the urethra and obstructs the urine outflow. The bladder no longer empties completely, creating an environment in which infections, bladder stones, and chronic prostatities may develop. If left untreated, chronic obstruction can lead to the back up of urine into the ureters and compromise kidney function. In hyperplastic prostate tissue, the prostate capsule, and the bladder neck are blocked, by using a a-adrenergic antagonist drugs; the smooth muscle tone of these structures is decreased. As a result, resistance to urinary flow through the bladder neck and the prostatic urethra decreases and urinary flow increases. A variety of a a-adrenergic antagonists with distinct properties have been investigated as possible treatments for benign prostate hyperplasia.
Pre-ADMET software derived information has significant value in the design of newer potent drug molecules. All these predicted data help us to screen the potent and safe compounds for further their synthesis with its biological evaluation. Benzothiazole is versatile heterocyclic rings associated with multiple biological activities that result to inspire continue developing of Benzothiazole analogues. The antidiabetic activity can be evaluated by inducing the diabetic conditions in the experimental model using streptozotocin (STZ). The present research work was focused on screening of potent Benzothiazole derivatives with the help of Pre ADMET toxicity profile and further evaluating their biological activity in the streptozotocin induced diabetes rat model. Among all the selected compounds 6e and 6f were found more potent for anti-diabetic activity at 350 mg/kg (p. o.).
Simple, accurate, economical, and reproducible UV spectrophotometric and column high-performance liquid chromatographic (HPLC) methods were developed for simultaneous estimation of a 2-component drug mixture of metoprolol tartrate and hydrochlorothiazide in combined tablet dosage form. The first method used the simultaneous equation method with 7 mixed standards and the absorption maxima at 223 and 271 nm, respectively, for metoprolol tartrate and hydrochlorothiazide in methanol. Linearity was observed in the concentration ranges of 424 and 216 g/mL for metoprolol tartrate and hydrochlorothiazide, respectively. The developed HPLC method used a reversed-phase C18 column and methanolwater (95 + 5) mobile phase at an ambient temperature of 27 2C and UV detection at 225 nm; the run time was 10 min, and quantification was based on peak area. The injection repeatability and intraday and interday repeatability were calculated. Paracetamol was used as an internal standard for the HPLC method, and linearity was observed in the concentration range of 550 g/mL for metoprolol and 220 g/mL for hydrochlorothiazide. The proposed methods were successfully applied for the determination of metoprolol tartrate and hydrochlorothiazide in bulk powder and dosage form. The results obtained were analyzed statistically, and there was no significant difference between the 2 methods. The validation was performed according to International Conference on Harmonization guidelines.
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