The aim of the research work was to develop and characterize a concanavalin-A (Con-A) conjugated gastroretentive multiparticulate delivery system of clarithromycin (CM) for the effective treatment of colonization of Helicobacter pylori (H. pylori). Ethylcellulose (EC) microspheres containing CM were prepared using emulsification/ evaporation method. Formulations were characterized for micromeritic properties, % drug entrapment, % yield, surface morphology, buoyancy behavior and in vitro drug release in simulated gastric fluid. EC microspheres of CM were conjugated with Con-A. IR spectroscopy and differential scanning calorimetry were used to confirm conjugation of Con-A to EC microspheres while Con-A conjugated microspheres were further characterized using the parameters of zeta potential, mucoadhesiveness to gastric mucosa and Con-A conjugation efficiency with microspheres. The gamma scintigraphy of the formulations was carried out in albino rabbits (New Zealand) to monitor the transit of Con-A conjugated EC microspheres and marketed formulation in gastrointestinal (GI) tract. The microparticles were found to be regular and spherical in shape. The particle size of microspheres was found to vary from 112.45 +/- 3.39 to 124.23 +/- 2.31 microm with polymer concentration from 1% w/v to 3% w/v. IR and DSC studies confirmed the attachment of Con-A with EC microspheres. All the microsphere formulations showed good % drug entrapment (70 +/- 3%). Zeta potential of EC microspheres and Con-A conjugated EC microspheres was found to be -8.77 +/- 0.5 mV and 7.56 +/- 0.7 mV, respectively. Maximum mucoadhesion (85 +/- 2.6%) was shown by Con-A conjugated EC microspheres as compared with nonconjugated EC microspheres (12.0 +/- 3.2%). Performance of developed formulation in GI tract was visualized successfully by gamma scintigraphy in rabbits. Prolonged gastric residence time (GRT) of over 6 h was achieved in all rabbits for Con-A conjugated microspheres of CM. It is concluded that designed targeted delivery system could possibly treat the colonization of H. pylori.
The aim of this work is to apply Box-Behnken design to optimize the transfersomes were formulated by modified rotary evaporation sonication technique using surfactant Tween 80. The response surface methodology was used having three-factored with three levels. The prepared formulations were characterized for vesicle shape, size, entrapment efficiency (%), stability, and in vitro permeation. The result showed that drug entrapment of 84.24% with average vesicle size of 35.41 nm and drug loading of 8.042%. Thus, optimized formulation was found good stability and is a promising approach to improve the permeability of apigenin in sustained release for prolonged period of time.
The aim of this study was to develop a potential novel formulation of carbopol-based nanoemulsion gel containing apigenin using tamarind gum emulsifier which was having the smallest droplet size, the highest drug content, and a good physical stability for Skin delivery. Apigenin loaded nanoemulsion was prepared by high speed homogenization method and they were characterized with respect to morphology, zeta potential, differential scanning calorimeter study, and penetration studies. In-vitro release studies and skin permeation of apigenin loaded nanoemulsion by goat abdominal skin was determined using Franz diffusion cell and confocal laser scanning microscope (CLSM). The cytotoxicity of the reported formulation was evaluated in HaCaT Cells (A) and A431 cells (B) by MTT assay. The nanoemulsion formulation showed droplet size, polydispersity index, and zeta potential of 183.31 nm, 0.532, and 31.9 mV, respectively. The nanoemulsions were characterized by TEM demonstrated spherical droplets and FTIR to ensure the compatibility among its ingredients. CLSM showed uniform fluorescence intensity across the entire depth of skin in nanocarriers treatment, indicating high penetrability of nanoemulsion gel through goatskin. The nanoemulsion gel showed toxicity on melanoma (A341) in a concentration range of 0.4-2.0 mg/ml, but less toxicity toward HaCaT cells. The carbopol-based nanoemulsion gel formulation of apigenin possesses better penetrability across goatskin as compared to marketed formulation. Hence, the study postulates that the novel nanoemulsion gel of apigenin can be proved fruitful for the treatment of skin cancer in near future.
The aim of present study was to develop the efficient targeting of Concanavalin-A conjugated nanotransfersomal gel to bind directly to melanocytes gel layer against UVB induced skin carcinoma. Carbopol loaded nanotransfersomal gel have prepared by modified rotary evaporation sonication technique & conjugated synthesized by carbodiimide method and they were characterized the morphology, zeta potential, penetration and cell viability. In vitro release studies & skin permeation have determined using Franz diffusion cell and confocal laser scanning microscope (CLSM). The conjugated formulation showed vesicles size, polydispersity index, zeta potential and % conjugation efficiency of 179.0 ± 0.32 nm, 0.197 ± 0.07, 35.1 ± 0.21 mV and 89.73 ± 1.29% respectively. The surface morphology was confirmed by transmission electron microscopy (TEM) and FTIR to make sure the compatibility among its ingredients. Con-A conjugated nanotransfersomal gel showed toxicity on melanoma (A375) in a concentration range of 0.4-2.0 mg/mL, but less toxicity toward HaCaT cells. The MTT assay has analyzed against two different cell lines, to determine their anti-cancer potentials and their targeting ability. Conjugated formulation were found to decrease the cell viability, higher skin targeting efficacy in invitro & in-vivo. Concanavalin conjugated nanotransfersomal gel of apigenin promise an efficient and economic approach for the skin cancer.
Alzheimer's disease (AD) is an accelerating neurodegenerative disorder, dementia in the world. Current treatments for Alzheimer's disease primarily focus on enhancement of cholinergic transmission & leading to neuronal dysfunction and loss in the brain. Flavonoid bioactive compounds are the major role for the designer of a new generation of therapeutic agents that are clinically effective in treating neurodegenerative diseases. Apigenin & quercetin are attractive biomarkers in this regards which has been epidemiological studies height a Neuroprotective and related to a lower risk of developing dementia or gradual decline its progressive. The continuing investigation of the potential preventive activity of quercetin and apigenin should be evaluated in long-term exposure clinical trials, using preparations with high bioavailability and promising to yield a possible remedy for this pervasive disease. Thus, the aim of the review, we analyzed the enhancing effects of apigenin and quercetin and discuss the potential of these compounds for Alzheimer's disease prevention and treatment.
Tuberculosis is an endemic disease in the developing countries worldwide. Early and definitive diagnosis of Active Pulmonary Tuberculosis (TB) is important both at individual and population level for reducing mortality as well as transmission of the disease. Currently available diagnostics can be broadly categorized into microscopy, culture based and molecular method-based approaches. Among the advanced molecular methods, the Nucleic Acid Amplification Test (NAA), Line Probe Assay and Cartridge Based Nucleic Acid Amplification Test (CB NAAT) are mentionable. However, all these diagnostic methods either have compromised sensitivity or require expensive instrumentations that ultimately limit their efficacy as established diagnostic method. Currently used rapid and affordable diagnostic test for TB is sputum microscopy that detects Mycobacterium tuberculosis (Mtb) in clinical sample. This test has sub-optimal sensitivity as it depends firstly on the abundance of Mtb in the sample and secondly on operator’s accuracy. On the other hand, culture-based diagnostic tests are time-consuming and dependent on expertise and infrastructure. Likewise, molecular tests are also dependent on expensive instrumentation and technical sophistication. Hence, rapid, sensitive and affordable diagnostic method for the detection of Active Pulmonary tuberculosis at an early phase is still a primary requisite.
Formulation & evaluation of Eclipta alba hydro-gel, the medicinal herbal hydrogel was prepared by using alcoholic extracted leaf powder of Eclipta alba, Carbopol-934, Acacia, Glycerin Sodium benzoate and HPMC. Leaves in concentration (1% and 5%) and evaluated using physiological measurements. The prepared herbal hydrogel formulation was studied for pre-liminary evaluation such as Viscosity, pH, Spreadibility, Rheological studies, Skin irritation test and Drug content uniformity Accelerated stability studies for 3 months. The Formulated hydrogel pH was found to range of 6.45 to 6.68, which lies in the normal pH range of the skin. The formulations did not produce any skin irritation, i.e., erythematic and edema for about a week, when applied over the skin. The viscosity of formulation was range 1024 which spread on the skin properly. On the basis of evaluation study, it can be concluded that Eclipta alba Linn. Medicinal herbal hydrogel may be used for wound healing, antibacterial and antifungal activity anticancer, Anti-inflammatory activity.
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