The aim of the present study is an attempt to formulate and evaluate Levofloxacin loaded solid lipid nanoparticles and to evaluate its antimicrobial activity against S. aureus. Solid lipid nanoparticle was prepared by hot homogenization followed by ultrasonication method using steric acid as lipid and poloxamer 188 as surfactant. Antimicrobial efficacy studies, Ocular irritation studies, stability studies were conducted for the selected formulations. Compatibility studies by FT-IR and DSC showed no significant interactions between drug and excipients. The comparative in-vitro study of the optimized formulation shows better release than the marketed product. The formulations were stable at intermediate stability testing conditions.Levofloxacin loaded SLN were successfully prepared by the hot homogenization method. The developed formulations were stable non irritant and showed better antibacterial action. From the above study we can conclude that the developed formulation is hence suitable for sustained ocular drug delivery having better antibacterial action.
Pavan kumar reddy A*, S. Parthiban, A. Vikneswari, G.P. Senthilkumar.
The present work is undertaken to explore more possibilities of finding β-lactam derivatives with enhanced anti-inflammatory activity. The scheme involves two steps. In the first step different Schiff bases are synthesized from 4-Amino antipyrine and six differently substituted aromatic aldehydes. In the second step, 2-azetidinone was synthesized by ketene-imine cyclization (Schrodinger) by adding chloroacetyl chloride. The lead compounds are docked against COX enzyme and it was calculated that the derivative AZ5 shows the best docking score which was compared with that of the in-vivo anti-inflammatory activity. It was found that the result of the anti-inflammatory activity correlated with the docking score of the concerned derivative.
The effective encapsulation of the drugs that are highly soluble in both aqueous and organic solvent are intricate to attain using standard nanoparticle preparation methods, such as nanoprecipitation (NPC) and double emulsion solvent evaporation method (DESE) due to the rapid partitioning of drug to the external aqueous phase. Modifications of standard methods are required to enhance the encapsulation efficiency. The present work focused on enhancing the encapsulation of highly aqueous and solvent soluble model drug rivastigmine tartrate. The prepared NP was evaluated for its physicochemical properties. The change of aqueous phase pH from 6-9 in NPC method showed encapsulation efficiency from 15 to 35% with the size of 125±12nm and potential ranged from -31±2 to -40±3mv. In DESE method the use of DCM: EA (50:50) as an organic phase resulted in 1 fold increase of encapsulation with the size of 175±15nm. When EA used as an organic phase it results in 2.5 folds increase in encapsulation efficiency. The NP prepared using Pluronic F-127 showed the zeta value (-13±2mv) while DMAB showed the zeta value (+ 40±1mv) with smaller size (105±10nm). In vitro release studies for NPC and DESE method for 24hr was 45.4 ±2.7 and 51.2±3.2 %. The cytotoxicity study using SH-SY-5Y cell line evidenced no toxicity of prepared NP.
TheAegle marmelos whole leaf powder (2000mg) and alcohol extract (400mg) chronic oral treatment for 90 days in male Wistar rats caused elevation of serum transaminases and alkaline phosphatases. This was maximum after 60 days of treatment this effect does not substantiate for a toxic impact on liver, as the levels have been found to come towards normalcy after 90 days of treatment and fluctuations in the serum total proteins were also noticed, but they were found to be within normal range. The blood urea and hematological parameters during different duration of treatment showed absence of fluctuations, which indicates no deleterious impact on vital tissues like liver, kidney and bone marrow; the post mortem observation and histopathology studies confirms this and thus it can be suggested that the fluctuations are due to initial stress and cannot be considered as reflection of any permanent toxic injury. These treatments showed a decrease in serum total cholesterol, triglycerides, VLDL, LDL with an increase in HDL. The β-sitosterol and Rutin are reported to posses’ hypocholesterolemic effect and the rutin was identified in the alcohol extract. The acute toxicity study of the leaf powder and extracts were non-toxic up to a dose of 2000 mg/ kg b. wt.
The aim of present study to evaluate antidiabetic activity of ethanolic extract of Tragia Bicolor MIQ. (Family: Euphorbiaceae) roots in streptozotocin induced diabetic rats. The alcoholic extract of Tragia Bicolor MIQ was studied for antidiabetic activity in streptozotocin induced diabetic rats by oral administration of extract 200&400mg/kg body weight for the period of 28 days. The preliminary phytochemical study showed the presence of flavonoids, carbohydrates and glycosides, phenolic compounds and tannins. From the toxicity study it was observed that ethanolic extract of Tragia Bicolor MIQ was nontoxic up to the dose of 2000mg/kg body weight. The determination of blood glucose level by GOD-POD kit method. The effect was compared with oral dose of 0.6mg/kg Glibenclamide. The result shows the alcoholic extract of Tragia Bicolor MIQ level significantly lowered the blood glucose of hyperglycemic rats in the dose dependent manner and it was also comparable to that of the standard drug glibenclamide.