Search

The objective was to develop a stable and non-compliance coated solid–lipid nanoparticles (coated SLN) using polymer (Eudragit L100) and lipoid (glycerol monostearate: soya lecithin) for partial dose reduction of isradipine [ISR; 2.5 mg by combination of bioenhancing agent (rutin; Ru) in equivalent ratio]. The physicochemical characterizations were performed by FT-IR and DSC of elected model drug (ISR), drug mixer with Ru/polymer and coated SLN with Ru (ONbp); the resulted distinctive peaks demonstrated that no chemical interaction and incompatibility found between them. The plasma samples of formulation (ONbp) were analyzed by liquid chromatography (HPLC) using UV-spectrometer. Data were integrated and analyzed with the help of a computer-designed program “Kinetica Software” (Thermo Scientific Kinetica, PK/PD Analysis, version 5.0, Philadelphia, PA). The pharmacokinetic study showed 3.2- to 4.7-folds enhancement in oral bioavailability of coated SLN of ISR with Ru (ONbp) when compared to a coated formulation of ISR without Ru (ONps) and conventional drug suspension. In vivo studies were revealed significantly at greater extent in (drug stability and solubility) oral absorption, which has shown potential entrapment efficiency (97.85% ± 1.02%) to improve biological activity against hypertension. Hence, nano-system of ISR against hypertension is achieved with consequent dose reduction with enhanced systemic bioavailability.

Background & objective Our research objective was to design, develop, optimize and characterize Granisetron HCl transdermal gel in order to minimize side effects associated with oral delivery. Method A statistical design was practically applied for further optimization and preparation of transfersomal gel using Box-Behnken methodology at three levels. The selected independent and dependent variables were Lipoid, surfactant and sonication time and encapsulation efficiency, size and flux correspondingly. Result The optimized formulation (GTV-16) morphology, shape, size, potential, encapsulation capacity and flux (using Franz-diffusion cell assembly via animal skin barricade medium) were determined. Then, GTV-16 incorporated into gel and during evaluation nano-transformal gel has good particle size of 127.7±1.08 nm, better entrapment efficiency of 83.0 ± 3.22 % and flux of 20.0 ± 1.88µgcm-2/h. Conclusion The results demonstrated that Granisetron Hydrochloride loaded nano-gel was significantly superior with 8.5 fold enhancement in bioavailability as compared with drug solution.

The objective was to develop a stable, reproducible and patient non-infringing novel transdermal drug delivery system “ nano-carrier transdermal gel ” (NCTG) in combination of partial dose replacement of diclofenac diethylamine (DDEA) by curcumin (CRM). The drug content of gel was 99.30 and 97.57% for DDEA and CRM. Plasma samples were analyzed by liquid chromatography with triple-quadrupole tandem mass spectrometer (LC–MS/MS). Data were integrated with Analyst™ and analyzed by WinNonlin ; stability parameters were analyzed using Tukey–Kramer multiple comparison test. Its average skin irritation scored 0.49 concluded to be non-irritant, safe for human use and in vivo studies revealed significantly greater extent of absorption and highly significant inhibition (%) of carrageenan induced paw edema. The results also demonstrated that encapsulation of drugs in nano-carrier increases its biological activity due to superior skin penetration potential. Hence, a novel once day transdermal gel of nano-carrier (nano-transfersomes; deformable vesicular) is achieved, to increase systemic availability, subsequent reduction in dose and toxicity of DDEA was developed for the treatment of inflammation.

The aim of the study was to develop and optimize Piroxicam transdermal gel formulation using three-factor, three-level Box-Behnken design by deriving a second-order polynomial equation to construct contour plots for prediction of responses as three selected independent variables with ratio of carbopol 974 (X1), ratio of propylene glycol (PG) (X2) and ratio of ethanol (X3). The dependent variables studied were the skin permeation rate of piroxicam (Y1), viscosity of the gel (Y2) and pH of the gel (Y3). Response surface plots were drawn, statistical validity of the polynomials was established to find the compositions of optimized formulation which was evaluated using the vertical Franz-type diffusion cell. The permeation rate of piroxicam increased proportionally with ethanol concentration but decreased with polymer concentration. The design demonstrated the role of the derived polynomial equation and contour plots in predicting the values of dependent variables for the preparation and optimization of gel formulation.

Our research objective was to optimize and design nano-biosystem of Isradipine (IDP) via novel bioenhancer (Rutin) loaded solid-lipid nanobioparticles (ANbp) using Taguchi design (TgD) methodology. Firstly, preliminary screening of solid lipid nanoparticles (SLNps) formulation core factors (A, B & C; Lipoid's, poly-acid, sonication time respectively at fixed dose of model drug were assessed on entrapment efficiency & particle size; R1 & R2) by performed experimentally of three factor three levels orthogonal L27 array. Consequently, signal to noise (S/N) ratio plot of responses were drawn to predict better quality fitted-levels of significant factor for eminence optimization. Further, optimized quality spaces composition was used via enhancer (Rutin) to design advanced bio-formulation (ANbp) and done its evaluation (entrapment efficiency, particle size, drug release & kinetics). As designed, ANbp results showed better sustained (86.54% as compared to control SLNps 94.48% in 24h) release, kinetics & stability behavior with good entrapment efficiency (97.58%) and desired smaller particle size (108nm). Therefore, statistically (TgD) optimization strategy would be considered to design nano-drug delivery system with bio-agent in-order to improve oral bioavailability of antihypertensive agents.

A reversed phase high performance liquid chromatographic (RP-HPLC) method using Symmetry C18, 5.0-µm column was developed for simultaneous determination of Diclofenac diethylamine (DDEA) and Curcumin (CRM). Mobile phase consisted of orthophosphoric acid 0.1% and acetonitrile (65:35), and the flow rate was 1.5 mL/min and elution was monitored initially at 425 nm for CRM, after 14.7 min wavelength was changed to 275 nm for detection of DDEA. Response was a linear function of concentration over the range 0.245–1.96 µg/mL (R2 = 0.9998) for DDEA and 55–445 ng/mL (R2 = 0.9992) for CRM and the limits of detection were 245.5 ng/mL for DDEA and 55.30 ng/mL for CRM. The limit of quantitation was 491.1 ng mL − 1 for DDEA and 165.87 ng mL − 1 for CRM. The method was validated in accordance with ICH guidelines. The method was used for simultaneous quantification of DDEA and CRM in transdermal gel formulations and to check content uniformity. The excipients present in the formulation did not interfere with the assay. T...

The aim of this study was to develop and optimize a transdermal gel formulation for Diclofenac diethylamine (DDEA) and Curcumin (CRM). A 3-factor, 3-level Box-Behnken design was used to derive a second-order polynomial equation to construct contour plots for prediction of responses. Independent variables studied were the polymer concentration (X(1)), ethanol (X(2)) and propylene glycol (X(3)) and the levels of each factor were low, medium, and high. The dependent variables studied were the skin permeation rate of DDEA (Y(1)), skin permeation rate of CRM (Y(2)), and viscosity of the gels (Y(3)). Response surface plots were drawn, statistical validity of the polynomials was established to find the compositions of optimized formulation which was evaluated using the Franz-type diffusion cell. The permeation rate of DDEA increased proportionally with ethanol concentration but decreased with polymer concentration, whereas the permeation rate of CRM increased proportionally with polymer concentration. Gels showed a non-Fickian super case II (typical zero order) and non-Fickian diffusion release mechanism for DDEA and CRM, respectively. The design demonstrated the role of the derived polynomial equation and contour plots in predicting the values of dependent variables for the preparation and optimization of gel formulation for transdermal drug release.

A new UV-Spectrophotometric method has been described for the simultaneous assay of Diclofenac Diethylamine and Curcumin in transdermal gels using methanol as the solvent. The method is based on simultaneous equation or Vierodt’s method. The λmax values for Diclofenac Diethylamine and Curcumin in the solvent medium were found to be 275 nm and 425 nm respectively. The systems obey Beer’s law in the range of 2.0 to 22.0 μg/ml and 1.0 to 6.0μg/ml with correlation coefficient of 0.9994 and 0.9998 for Diclofenac Diethylamine and Curcumin respectively. Repeatability, Interday and intraday precision were found to be 1.61, 0.586, 0.662 and 0.371, 0.374, 0.410 respectively. Results of analysis have been validated statically and by recovery studies.

The aim of this study was to design and optimize a nano-transfersomes of Diclofenac diethylamine (DDEA) and Curcumin (CRM). A 3(3) factorial design (Box-Behnken) was used to derive a polynomial equation (second order) to construct 2-D (contour) and 3-D (Response Surface) plots for prediction of responses. The ratio of lipid to surfactant (X1), weight of lipid to surfactant (X2) and sonication time (X3) (independent variables) and dependent variables [entrapment efficiency of DDEA (Y1), entrapment efficiency of CRM (Y2), effect on particle size (Y3), flux of DDEA (Y4), and flux of CRM (Y5)] were studied. The 2-D and 3-D plots were drawn and a statistical validity of the polynomials was established to find the compositions of optimized formulation. The design established the role of the derived polynomial equation, 2-D and 3-D plots in predicting the values of dependent variables for the preparation and optimization of nano-transfersomes for transdermal drug release.