Applying response surface methodology to optimize nimesulide permeation from topical formulation

Shahzad, Yasser; Afreen, Urooj; Shah, Syed Nisar Hussain; Hussain, Talib

doi:10.3109/10837450.2012.723721

Cited by 27 publications

(24 citation statements)

References 28 publications

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“…Number of thiol contents per gram of the TARX were determined by the quantification of thiol substituents using the Ellman’s reagent method [20, 21]. 0.5%, w/v dispersions of ARX (control) and TARX (sample) were prepared and diluted with 0.5 M phosphate buffer of pH 8.0 to a concentration of 0.15% w/v.…”

Section: Methodsmentioning

confidence: 99%

Thiolation of arabinoxylan and its application in the fabrication of controlled release mucoadhesive oral films

Hanif

Zaman

2017

DARU J Pharm Sci

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BackgroundMucoadhesion is an important property that helps oral drug delivery system to remain attached with buccal mucosa and hence to improve the delivery of the drug. The current study was designed to achieve the thiol modification of Arabinoxylan (ARX) and to develop a mucoadhesive oral film for the improved delivery of tizanidine hydrochloride (TZN HCl).MethodSynthesis of thiolated arabinoxylan (TARX) was accomplished by esterification of ARX with thioglycolic acid (TGA). TARX was further used for the development of mucoadhesive oral films which were prepared by using a solvent casting technique. Formulation of the films was designed and optimized by using central composite design (CCRD), selecting TARX (X1) and glycerol (X2) as variables. Prepared film formulations were evaluated for mechanical strength, ex-vivo mucoadhesion, in-vitro drug release, ex-vivo drug permeation, surface morphology and drug contents.ResultsThiolation of ARX was confirmed by fourier transform infra-red spectroscopy (FTIR) as a peak related to thiol group appeared at 2516 cm−1. The claim of successful thiolation of ARX was strengthened by the presence of 2809.003 ± 1.03 μmoles of thiol contents per gram of the polymer, which was determined by Ellman’s reagent method. From the results, it was observed that the films were of satisfactory mechanical strength and mucoadhesiveness with folding endurance greater than 300 and mucoadhesive strength 11.53 ± 0.17 N, respectively. Reasonable drug retention was observed during in-vitro dissolution (85.03% cumulative drug release) and ex-vivo permeation (78.90% cumulative amount of permeated drug) studies conducted for 8 h. Effects of varying concentrations of both polymer and plasticizer on prepared mucoadhesive oral films were evaluated by ANOVA and it was observed that glycerol can enhanced the dissolution as well as permeation of the drug while TARX has opposite impact on these parameters.ConclusionIn nutshell, TARX in combination with glycerolwas found to be suitable for the development of controlled release mucoadhesive oral films of TZN HCl.Graphical AbstractSchematic diagram showing conversion of ARX to TARX, TARX to oral film and evaluation of fabricated oral film

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Section: Methodsmentioning

confidence: 99%

Thiolation of arabinoxylan and its application in the fabrication of controlled release mucoadhesive oral films

Hanif

Zaman

2017

DARU J Pharm Sci

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“…PG and SLS were used as permeation enhancer as per protocol of “Response Surface Methodology” (as enlisted in Table 2). This methodology was deployed to optimize topical formulations 19. These formulations were tested against full range of parameters, for instance, pH, temperature stability tests in 8°C±0.1°C, 25°C±0.1°C and 40°C±0.1°C and physical properties such as color, bleeding (separation of liquid) and rheology.…”

Section: Methodsmentioning

confidence: 99%

Fabrication of anti-vitiligo ointment containing <em>Psoralea corylifolia</em>: in vitro and in vivo characterization

Hussain¹,

Hussain²,

Manan³

et al. 2016

DDDT

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BackgroundVitiligo is a repugnant and odious dermatological malady of the time. It has an detrimental impact on the pigmentation of the human skin as a result of the destruction of cutaneous melanocytes. It affects 1%–2% of the population worldwide. Different therapeutic regimens have been deployed to treat vitiligo, but none of them could stand alone to be stated as a perfect cure. Recently, a change has been observed through novel experimental-designed optimization leading to the development of an anti-vitiligo ointment containing Psoralea corylifolia (PC) seed powder.AimThe aim of this study was to explore the clinical outcomes of ointment containing powdered seeds of PC.Materials and methodsGuided by the protocol Response Surface Methodology, 13 formulations of concentration variance of permeation enhancers were prepared. The formulation fulfilling the required criteria (pH; temperature stability tests at 8°C±0.1°C, 25°C±0.1°C and 40°C±0.1°C; and the physical properties such as color, bleeding and rheology) was selected for clinical trials. Fourier transform infrared spectroscopy studies of seed powder of PC and selected formulation of the seed powder were performed. After obtaining informed consents and with prior approval of university and hospital ethical review boards, 20 patients (age range 25–65 years) were included in the present study. Formulations were applied on the affected body parts of patients, and some affected portion of the same patient was taken as control (self-control study design). The pigmentation of white spots of vitiligo was photographically evaluated before, during and after 12 weeks of treatment. Analysis of the measured values was performed using GraphPad Prism version 5 statistical software. A paired sample t-test was performed to observe variation between repigmented patches and white patches of self-control.ResultsHydrophilic ointment (10% w/w) prepared with seed powder of PC was fabricated. The ointment was found effective for small circular white lesions of vitiligo as compared to self-control. Pre- and post-treatment differences in the levels of pigmentation were statistically significant (P≤0.05).ConclusionOintment containing seed powder of PC could be an effective monotherapy for small circular white lesions of vitiligo.

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“…The mathematical form of the MLRA model is given as [9,25,26] where, β 0 , the intercept (demonstrating the mathematical mean of all numerical outcomes of 13 trials), β 1 and β 2 were the coefficients (calculated from the observed experimental values of Y), and X 1 and X 2 were coded levels of the independent variable(s). Polynomial equation, including interaction and quadratic factors were studied for all the response variables using the multiple linear regression analysis (MLRA) approach.…”

Section: Optimization Data Analysis and Numerical Optimizationmentioning

confidence: 99%

In vitro and ex vivo assessment of hydrophilic polymer‐ and plasticizer‐based thin buccal films designed by using central composite rotatable design for the delivery of meloxicam

Zaman

Hanif

2017

Adv Polym Technol

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The purpose of the study was to design a dosage form with ability to deliver drug immediately, hence providing rapid relief in certain pain ailments. Meloxicam (MLX) was selected as a model drug and buccal films were designed by using the solvent casting technique. A central composite rotatable design (CCRD) was used as a statistical tool to design and optimize the film formulations. No noticeable interaction was found between the drug and polymer when they were subjected to Fourier transform infrared spectroscopy (FTIR). Scanning electron microscopy (SEM) revealed the smooth surface of the film and uniform mixing of drug and polymer.X-ray diffractometry (XRD) was carried out to observe crystalline and amorphous nature of meloxicam. Differential scanning calorimetric (DSC) analysis was used to investigate the thermal behavior of free drug and drug-loaded formulation. The prepared film showed good mechanical property as folding endurance was found to be greater than 100 in all formulations. The cumulative drug release was found to be more than 80% in initial at dissolution time of 5 min, when the prepared films were subjected to dissolution studies in phosphate buffer at pH 6.8. Thus, it can be concluded that the hydrophilic polymer and plasticizer have definite impact on formulation and characteristics of rapidly dissolving buccal films and have the ability to prepare a suitable immediate release buccal film of meloxicam. K E Y W O R D Sbuccal films, drug delivery system, ex-vivo permeation, hydrophilic polymer, meloxicam, plasticizer, solvent casting method

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Applying response surface methodology to optimize nimesulide permeation from topical formulation

Cited by 27 publications

References 28 publications

Thiolation of arabinoxylan and its application in the fabrication of controlled release mucoadhesive oral films

Thiolation of arabinoxylan and its application in the fabrication of controlled release mucoadhesive oral films

Fabrication of anti-vitiligo ointment containing <em>Psoralea corylifolia</em>: in vitro and in vivo characterization

In vitro and ex vivo assessment of hydrophilic polymer‐ and plasticizer‐based thin buccal films designed by using central composite rotatable design for the delivery of meloxicam

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