D-Optimal Mixture Design: Optimization of Ternary Matrix Blends for Controlled Zero-Order Drug Release From Oral Dosage Forms

El-Malah, Yasser; Nazzal, Sami; Khanfar, Nile M.

doi:10.1080/03639040600685167

Cited by 49 publications

(21 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The one-factor-at-a-time optimization also ignores interaction between factors and may call for an unnecessarily large number of runs. 9 Currently more and more attention has been paid to the formulation optimization in the course of establishing SLN dispersion systems. Some studies [10][11][12] have optimized nanoparticulate formulations using factorial design.…”

mentioning

confidence: 99%

Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design

Hao

Fang²,

Zhou³

et al. 2011

IJN

View full text Add to dashboard Cite

The purpose of the present study was to optimize a solid lipid nanoparticle (SLN) of chloramphenicol by investigating the relationship between design factors and experimental data using response surface methodology. A Box-Behnken design was constructed using solid lipid ( X 1 ), surfactant ( X 2 ), and drug/lipid ratio ( X 3 ) level as independent factors. SLN was successfully prepared by a modified method of melt-emulsion ultrasonication and low temperature-solidification technique using glyceryl monostearate as the solid lipid, and poloxamer 188 as the surfactant. The dependent variables were entrapment efficiency (EE), drug loading (DL), and turbidity. Properties of SLN such as the morphology, particle size, zeta potential, EE, DL, and drug release behavior were investigated, respectively. As a result, the nanoparticle designed showed nearly spherical particles with a mean particle size of 248 nm. The polydispersity index of particle size was 0.277 ± 0.058 and zeta potential was −8.74 mV. The EE (%) and DL (%) could reach up to 83.29% ± 1.23% and 10.11% ± 2.02%, respectively. In vitro release studies showed a burst release at the initial stage followed by a prolonged release of chloramphenicol from SLN up to 48 hours. The release kinetics of the optimized formulation best fitted the Peppas–Korsmeyer model. These results indicated that the chloramphenicol-loaded SLN could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release.

show abstract

mentioning

confidence: 99%

Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design

Hao

Fang²,

Zhou³

et al. 2011

IJN

View full text Add to dashboard Cite

show abstract

“…The mixture components cannot range in an independent way since their sum has to be equal to 100% [18] . D-optimal mixture design is commonly used to reveal main effects and interaction effects between the independent variables of the experiment [20] .…”

Section: D-optimal Designmentioning

confidence: 99%

D-optimal Design and Development of Microemulsion Based Transungual Drug Delivery Formulation of Ciclopirox Olamine for Treatment of Onychomycosis

Chouhan¹,

Saini²

2016

ijps

View full text Add to dashboard Cite

The objective of the present study was to design and develop a microemulsion based transungual drug delivery formulation of ciclopirox olamine using colloidal carrier for treatment of onychomycosis. Capmul PG8 was selected as oil phase due to the high solubility of ciclopirox in it as compared to other oils and Cremophor EL and Transcutol P were used as surfactant and cosurfactant respectively. Pseudoternary phase diagrams were constructed using different ratio of S mix (surfactant:cosurfactant). The phase diagram obtained from 1:3 ratio showed largest microemulsion region. The construction of microemulsion was further optimized by D-optimal mixture design, taking oil, S mix and water as independent variables and globule size, transungual flux, and nail drug loading as response variables. Mathematical equations and response surface plots were used to correlate the dependent and independent variables. The optimized composition of microemulsion was predicted by numerical optimization technique on the basis of the highest desirability value. The predicted optimized microemulsion which contained 2% oil, 40% S mix , and 58% water was incorporated into Carbopol 940 The human nail plate is the most resistant barrier of the nail structure for drug penetration and therefore it is very difficult to deliver drug through nail in transungual infections [1] . Onychomycosis, also known as tinea unguium, is the most common nail fungal disease affecting approximately 14% of the general population and 48% aged population [2][3][4] . It affects one or more components of nail apparatus, including the nail plate, the nail matrix, and the nail bed.In the treatment of onychomycosis, the oral antifungal drug therapy remains the only choice due to deepseated persistent nature of the infectious fungi and limitation of topical route of drug administration due to poor drug permeation through nail plate [5,6] . A longduration oral antifungal therapy is, however, required to achieve therapeutic drug concentration in nail plate due to limited blood circulation at this site. This is often associated with serious side effects, drug interactions, and high recurrence rates. The problem of adverse effects of oral antifungal drug therapy can only be overcome if the drug delivery through nail plate could be realized [6] .The human nail plate is a highly ordered and dense epidermal structure grossly made up of three distinct layers -a thin dorsal lamina, the thicker intermediate lamina, and a ventral layer from the nail bed ( fig.1a). It composed of ~80% sulfur-rich α-keratin, 10-30%

show abstract

“…Traditional formulation screening and optimization process like univariate one-factor-at-a-time methods, however, may call for an unnecessarily large number of runs or give an unreliable result (El-Malah et al, 2006;Hao et al, 2011). Statistical experimental designs including Plackett-Burman and response surface methodologies can collectively eliminate these limitations of a singlefactor optimization process.…”

Section: Introductionmentioning

confidence: 99%

Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improvedin vivooral bioavailability andin situintestinal absorption of curcumin

Tang

et al. 2014

Drug Delivery

134

View full text Add to dashboard Cite

Purpose: The present study was to formulate curcumin solid lipid nanoparticles (Cur-SLNs) with P-gp modulator excipients, TPGS and Brij78, to enhance the solubility and bioavailability of curcumin. Methods: The formulation was optimized by Plackett-Burman screening design and Box-Behnken experiment design. Then physiochemical properties, entrapment efficiency and in vitro release of Cur-SLNs were characterized. In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of Cur-SLNs on the bioavailability and intestinal absorption of curcumin. Results: The optimized formulations showed an average size of 135.3 ± 1.5 nm with a zeta potential value of À24.7 ± 2.1 mV and 91.09% ± 1.23% drug entrapment efficiency, meanwhile displayed a sustained release profile. In vivo pharmacokinetic study showed AUC 0!t for Cur-SLNs was 12.27-folds greater than curcumin suspension and the relative bioavailability of Cur-SLNs was 942.53%. Meanwhile, T max and t 1/2 of curcumin for Cur-SLNs were both delayed comparing to the suspensions (p50.01). The in situ intestinal absorption study revealed that the effective permeability (P eff ) value of curcumin for SLNs was significantly improved (p50.01) comparing to curcumin solution. Conclusion: Cur-SLNs with TPGS and Brij78 could improve the oral bioavailability and intestinal absorption of curcumin effectively. KeywordsCurcumin, in situ intestinal absorption, oral bioavailability, P-glycoprotein, solid lipid nanoparticles History

show abstract

D-Optimal Mixture Design: Optimization of Ternary Matrix Blends for Controlled Zero-Order Drug Release From Oral Dosage Forms

Cited by 49 publications

References 19 publications

Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design

Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design

D-optimal Design and Development of Microemulsion Based Transungual Drug Delivery Formulation of Ciclopirox Olamine for Treatment of Onychomycosis

Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improvedin vivooral bioavailability andin situintestinal absorption of curcumin

Contact Info

Product

Resources

About