scholarly journals Formulation and Development of Stable Metaxalone Nanosuspension Using 32 Factorial Design

2016 ◽  
Vol 8 (04) ◽  
Author(s):  
Paras R. Vasanani ◽  
L. Patel ◽  
Chetan Detroja
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Surfactant Concentration ◽  
Class Ii ◽  
Poloxamer 407 ◽  
Saturation Solubility ◽  
Poor Solubility ◽  
Bcs Class Ii ◽  
Stirring Time ◽  
32 Factorial Design

Nanosuspensions are the dispersions of nanosized particles in a suitable vehicle prepared using surfactants or solubilizers to aid in nanosize distribution. Nanosuspension is best suited for dosage form development of poorly soluble drugs. According to the biopharmaceutical classification system, drugs with poor solubility fall either in BCS class II or BCS class IV. BCS class II drugs show poor solubility and good permeability; hence their bioavailability problems can be overcome by improving their solubility. Metaxalone is one such BCS class II drug from an oxazolidin-2-one class of centrally acting muscle relaxant drugs, indicated for relief of discomforts associated with acute, painful musculoskeletal conditions. Therefore, in present investigation, nanosuspension of Metaxalone has been formulated as an attempt to improve solubility and hence the overall bioavailability of Metaxalone. Media milling technique has been employed for nanosuspension preparation. Surfactant concentration (Poloxamer 407) and stirring time has been optimized using 32 factorial design to achieve desired particle size and saturation solubility responses as dependent variables. The particle size (PS) of 215.3 nm and maximum saturation solubility (SS) of 2805μg/ml was obtained as suggested solutions from factorial design which was further confirmed using check point analysis. Interaction of surfactant concentration and stirring time and their effect on particle size and saturation solubility was predicted using the contour plots and response surface plots. The optimized formulation showed around 99% metaxalone in vitro dissolution in comparison to around 46% dissolution from SKELAXIN® tablet at 30 minutes. These methodologies could therefore be employed successfully to improve solubility of any BCS class II drug and to predict effects and interactions of many experimental variables at the same time.

Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 32 factorial design

RSC Advances ◽  
2015 ◽  
Vol 5 (45) ◽  
pp. 35391-35404 ◽  
Author(s):  
Umme Hani ◽  
Gokul Krishna ◽  
H. G. Shivakumar
Keyword(s):  
Factorial Design ◽  
Class Ii ◽  
Anacardium Occidentale ◽  
Vaginal Candidiasis ◽  
Design And Optimization ◽  
Bcs Class Ii ◽  
32 Factorial Design

Clotrimazole (CTZ), a BCS class II drug, is widely employed in the treatment of vaginal candidiasis.

Formulation Development of Aceclofenac Loaded Nanosupension by Three Square (32) Factorial Design

2012 ◽  
Vol 4 (4) ◽  
pp. 1575-1583
Author(s):  
Atul A Patak ◽  
Jorwekar, P ◽  
P D Chaudhari
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
In Vivo Studies ◽  
Differential Scanning Calorimetric ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Calorimetric Analysis ◽  
32 Factorial Design

In the present study, aceclofenac loaded polymeric nanosuspension were formulated and evaluated.  Aceclofenac is a potent analgesic under BCS Class II. Due to the need for its frequent dosing, aceclofenac is an ideal candidate for sustained or controlled drug delivery. For optimization of prepared formulation, the three square (32) factorial design was used.  Tween 80 (X1) and combination of Eudragit RL 100 and RS 100 (X2) were used as independent variables and particle size (Y1), entrapment efficiency (Y2), and Percent drug release (Y3) were taken as dependent variables. The formulations were evaluated for particle size, zeta potential and drug entrapment. The in vitro drug release profile supports nanosuspension form to be used as a sustained release vehicle for aceclofenac. The formulation was characterized by differential scanning calorimetric analysis, in vivo studies and stability testing.

Novel Solid Forms of Insomnia Drug Suvorexant with Improved Solubility and Dissolution: Accessing Salts from Salt-Solvates Route

CrystEngComm ◽  
2021 ◽  
Author(s):  
Suman Gundlapalli ◽  
Ramesh Devarapalli ◽  
Ramesh Reddy Mudda ◽  
Ramanaiah Chennuru ◽  
Ravi Chandra Babu Rupakula
Keyword(s):  
Receptor Antagonist ◽  
Classification System ◽  
Class Ii ◽  
Biopharmaceutics Classification System ◽  
High Permeability ◽  
Poor Solubility ◽  
Bcs Class Ii ◽  
Biopharmaceutics Classification

Suvorexant (SRX) is a dual orexin receptor antagonist used for the treatment of insomnia. It belongs to the Biopharmaceutics Classification System (BCS) class-II with high permeability and poor solubility in...

scholarly journals Formulation and Optimization of Nanosuspension Prepared By Media Milling Technique to Enhance the Solubility of Isradipine

2017 ◽  
Vol 9 (04) ◽  
Author(s):  
Umang Motka ◽  
Mahesh Dabhi ◽  
Navin Sheth ◽  
Ashvin Dudhrejiya
Keyword(s):  
Particle Size ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Particle Size Reduction ◽  
Saturation Solubility ◽  
Lattice Design ◽  
Media Milling ◽  
Stirring Time ◽  
Selection Of

Isradipine is a poorly water soluble antihypertensive drug has low bioavailability. The aim of this study was to formulate and characterize isradipine nanosuspension to enhance the solubility of isradipine and thus its bioavailability. Media milling technique was used for the formulation of nanosuspension. The effects of different important process parameters, i.e. the selection of stirring time, selection of concentration of zirconium beads, stirring speed were investigated by preliminary studies while concentration of stabilizers were optimized by simplex lattice design. Concentration of HPMC E3 LV(X1), Carbopol 934P(X2) and PVP K25(X3) were selected as the independent variables whereas mean particle size (Y1), saturation solubility (Y2) and cumulative percentage drug release (cpr) (Y3) were selected as dependent variables. The optimized batch had 100% w/v of zirconium beads, 0.5%w/v of PVP K25 as stabilizer, 0.1%w/v of isradipine, 15 ml of distilled water and 20 hours of stirring time. The particle size and zeta potential of optimized nanosuspension were 248.6 ± 20 nm and 13.96 ± 5 mV respectively. The size of particles of nanosuspension was measured by particle size analyser and transmission electron microscopy (TEM). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) analysis indicated that there was no interaction between drug and stabilizers. The saturation solubility and in vitro dissolution rate of isradipine was significantly increased by particle size reduction and which may leads to increase the bio-availability of the Isaradipine. The stability study of the formulation was carried out for a period of 12 months.

scholarly journals Formulation and In Vitro Characterization of Raloxifene Nanostructured Lipid Carriers For Oral Delivery With Full Factorial Design-Based Studies Using Quality By Design (QbD) Approach

2020 ◽  
Vol 11 (4) ◽  
pp. 6417-6427
Author(s):  
Chintamani Panda ◽  
Sachinkumar Prabhubhai Chauhan ◽  
Krishnan Balamurugan
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Dissolution Rate ◽  
Surfactant Concentration ◽  
Quality By Design ◽  
Full Factorial Design ◽  
Nanostructured Lipid Carriers ◽  
Solid Lipid ◽  
Lipid Ratio ◽  
Full Factorial

The main aim of the present study is to improve the dissolution rate of Raloxifene Hydrochloride by formulating nanostructured lipid carriers (NLC) using Quality by Design (QbD) approach. The formulations of NLC-RH were prepared by the ultrasonication method using stearic acid as solid lipid, medium-chain triglyceride as the liquid lipid and polysorbate 80 as the surface-active agent. Two most critical quality attributes (CQAs) for NLC-RH were particle size and entrapment efficiency. The other attributes of medium influence identified includes dissolution rate, zeta potential and particle size didtribution. The Critical Material Attributes (CMAs) identified were solid lipid/liquid lipid ratio and surfactant concentration. The time required for ultrasonication was selected as a Critical Process Parameter (CPP). The 23 full factorial design was used to evaluate the relationship between the CMAs and CPPs variable. Based on the experiments, the composition of the optimal formulation is achieved with solid lipid/liquid lipid ratio of 7:3 and 7 % of surfactant concentration with 15 min of ultrasonication time. The optimized formulation of NLC-RH was found to be with a mean particle size of 146 nm with narrow particle size distributions. From the above results, it is concluded that a promising Raloxifene HCl loaded NLC could give a novel and potential therapy for osteoporosis.

Development of Rifampicin Nanoparticles by 32 Factorial Design

2010 ◽  
Vol 3 (3) ◽  
pp. 1085-1091
Author(s):  
Gambhire Makarand ◽  
Vaishali Gambhire ◽  
Bhalekar Mangesh
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
Chemical Interaction ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Sustained Drug Release ◽  
32 Factorial Design

The preparation and physico-chemical evaluation of rifam-picinloaded poly-(lactic-co-glycolic) acid (PLGA) nanoparticles as per 32 Factorial Design are presented. PLGA (X1) and PVA (Polyvinyl alcohol) solution (X2) as a stabilizing agent were used as independent variables where Particle size (PS) (Y1), Entrapment Efficiency (EE) (Y2) and % Drug Release at 12th h (REL)(Y3) were taken as dependant variables. Rifampicin nanoparticles were prepared by multiple emulsion solvent evaporation method. The results showed the method as reproducible, easy and efficient is the entrapment of drug as well as formation of spherical nanoparticles. Effect of polymer concentration was also evaluated with respect to their % drug entrapment efficiency. The in vitro release studies indicated the rifampicin-loaded PLGA nanoparticles provide sustained drug release over a period of 12h. The optimum batch was R3 which shown particle size 326 nm, 61.70 % EE and 57. 50% drug release at 12th h. Infrared spectroscopy analysis revealed that there was no known chemical interaction between drug and polymer. Hence, this investigation demonstrated the potential of the experimental design in understanding the effect of the formulation variables on the quality of rifampicin nanoparticles.

scholarly journals OPTIMIZATION AND IN VITRO EVALUATION OF THE RELEASE OF CLASS II DRUG FROM ITS NANOCUBOSOMAL DISPERSION

2019 ◽  
pp. 86-90
Author(s):  
Sadeq Jaafar Al-sakini ◽  
Nidhal Khazaal Maraie
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Poloxamer 407 ◽  
In Vitro Test ◽  
Surfactant Mixtures ◽  
Onset Of Action

Objective: This work involves investigation and evaluation of the factors that affect the preparation and the release of the model class II drug (erythromycin) to optimize the efficiency of its prepared nanocubosomal dispersion to give very fast initial burst effect within the first hour that can continue for further two hours. Methods: The work involved preparation of ten formulas of cubosomal dispersion by emulsifying different concentrations of glyceryl monooleate (GMO) (lipid content)/surfactant mixtures which were nano-sized and characterized morphologically by Transmission electronic microscopic (TEM), zeta potential, particle size, polydispersity index (pdI), pH, entrapment efficiency, conductivity test, dilution test and in vitro drug release. Results: The selected nanocubosomal formula (F1) showed pH (7.41), particle size (315.05 nm), pdI (0.194), zeta potential (-30.852), entrapment efficiency (91%) and gave a 70% drug release within the first hour of the in vitro test and continued until it gave 96.3% drug release with further 2 h. Conclusion: this work succeeded in preparing optimized cubosomal dispersion for erythromycin using different GMO/poloxamer 407 percent. The optimum formula gave an immediate release of the model drug (erythromycin) and it was ready to be incorporated in any suitable dosage form to give fast onset of action.

scholarly journals Formulation Characterization And Invitro, Invivo Evaluation Of Stabilized Rosuvastatin Calcium Nanosuspension

2020 ◽  
Vol 11 (2) ◽  
pp. 2657-2664
Author(s):  
Santhosh Raja M ◽  
Venkataramana K
Keyword(s):  
Particle Size ◽  
Class Ii ◽  
Nano Particles ◽  
Precipitation Method ◽  
Pharmacokinetic Parameters ◽  
Bcs Class Ii ◽  
Precipitation Technique ◽  
Nanoparticle Preparation ◽  
Rosuvastatin Calcium ◽  
Pvp K30

Rosuvastatin calcium is a BCS class II drug which is used as hyper lipidemic. Many of BCS class II drugs offer the disadvantage of solubility, to overcome the issue of solubility nanoparticle preparation is an promisable approach. A simple and efficient technique for the preparation of nanoparticles is precipitation technique. Polymeric nano particles have been prepared by employing nano precipitation technique. The nanosuspensions were prepared by using PVP K30, HPMC K15M, Eudragit L100 in various ratios using precipitation technique. The compatibility between the drug and various ingredients are tested by DSC. The formed nanoparticles were evaluated for various testing parameters like particle size, zetapotential, drug content and dissolution testing. Among all the formulations the nanosuspension prepared with Eudragit L 100 showed better characteristics. The dissolution test showed the drug release for 12 hours. The best formulation showed the particle size of 100.5 ± 5.4 nm and zeta potential of -55.1 mv. The invivo studies on the wistar rats showed better pharmacokinetic parameters when compared to the pure drug. Nano precipitation method was successfully employed to prepare Rosuvastatin calcium nanosuspension to improve the dissolution as well as bioavailability.

Application of Plakett-Burman Screening Design in Optimization of Process Parameters for Formulation of Canaglifozin Nanosuspension

2020 ◽  
Vol 13 (6) ◽  
pp. 5208-5216
Author(s):  
Nisha Patel ◽  
Hitesh A Patel
Keyword(s):  
Particle Size ◽  
Particle Diameter ◽  
Spherical Shape ◽  
Water Soluble ◽  
Pareto Chart ◽  
Independent Variables ◽  
Mean Particle Size ◽  
Screening Design ◽  
Stirring Time ◽  
Response Variables

In this study, we sought to improve the dissolution characteristics of a poorly water-soluble BCS class IV drug canaglifozin, by preparing nanosuspension using media milling method. A Plackett–Burman screening design was employed to screen the significant formulation and process variables. A total of 12 experiment were generated by design expert trial version 12 for screening 5 independent variables namely the amount of stabilizer in mg (X1), stirring time in hr (X2), amt of Zirconium oxide beads in gm (X3), amount of drug in mg (X4) and stirring speed in rpm (X5) while mean particle size in nm (Y1) and drug release in 10 min. were selected as the response variables. All the regression models yielded a good fit with high determination coefficient and F value. The Pareto chart depicted that all the independent variables except the amount of canaglifozin had a significant effect (p<0.001) on the response variables. The mathematical model for mean particle size generated from the regression analysis was given by mean particle size = +636.48889 -1.28267 amt of stabilizer(X1) -4.20417 stirring time (X2) -7.58333 amt of ZrO2 beads(X3) -0.105556 amt of drug(X4) -0.245167 stirring speed(X5) (R2=0.9484, F ratio=22.07, p<0.001). Prepared canaglifozin nanosuspension exemplified a significant improvement (p<0.05) in the release as compared to pure canaglifozin and marketed tablet with the optimum formulation releasing almost 80% drug within first 10min. Optimized nanosuspension showed spherical shape with surface oriented stabilizer molecules and a mean particle diameter of 120.5 nm. There was no change in crystalline nature after formulation and it was found to be chemically stable with high drug content.

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