Combined mixture-process variable approach: a suitable statistical tool for nanovesicular systems optimization

Habib, Basant A; AbouGhaly, Mohamed H.H.

doi:10.1517/17425247.2016.1166202

Cited by 22 publications

(12 citation statements)

References 48 publications

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“…Additionally, to ascertain the validity of the suggested models, the 95% two-sided prediction intervals (95% PIs) for the predicted values were calculated and all measured values for each response were assessed to find whether they fall within the 95% PIs or not (Habib and AbouGhaly, 2016 ). Desirability function approach (DF) was applied by the Design ® expert software in order to simultaneously compromise the several conflicting response variables to attain optimum formulations that best satisfy the predetermined constraints previously listed in Table 1 (Park and Park, 1998 ).…”

Section: Methodsmentioning

confidence: 99%

Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization

2018

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Keratomycosis is a serious corneal disease that can cause a permanent visual disability if not treated effectively. Sertaconazole nitrate (STZ), a novel broad spectrum antifungal drug, was suggested as a promising treatment. However, its utility in the ocular route is restricted by its poor solubility, along with other problems facing the ocular delivery like short residence time, and the existing corneal barrier. Therefore, the objective of this study was to formulate STZ loaded binary mixed micelles (STZ-MMs) enriched with different penetration enhancers using thin-film hydration method, based on a 31.22 mixed factorial design. Different formulation variables were examined, namely, type of auxiliary surfactant, type of penetration enhancer, and total surfactants: drug ratio, and their effects on the solubility of STZ in MMs (SM), particle size (PS), polydispersity index (PDI), and zeta potential (ZP) were evaluated. STZ-MMs enhanced STZ aqueous solubility up to 338.82-fold compared to free STZ. Two optimized formulations (MM-8 and MM-11) based on the desirability factor (0.891 and 0.866) were selected by Design expert® software for further investigations. The optimized formulations were imaged by TEM which revealed nanosized spherical micelles. Moreover, they were examined for corneal mucoadhesion, stability upon dilution, storage effect, and ex vivo corneal permeation studies. Finally, both in vivo corneal uptake and in vivo corneal tolerance were investigated. MM-8 showed superiority in the ex vivo and in vivo permeation studies when compared to the STZ-suspension. The obtained results suggest that the aforementioned STZ loaded mixed micellar system could be an effective candidate for Keratomycosis-targeted therapy.

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Section: Methodsmentioning

confidence: 99%

Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization

2018

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“…The proposed design in this study allows for the fitting of up to a quadratic model with three df for lack of fit or special cubic with only two df for lack of fit. The initial models suggested by the program were further manually improved case-by-case aiming at increasing the adjusted R 2 and the prediction R 2 with a non-significant model lack of fit (Gonnissen et al., 2008 ; Pat & Wayne, 2014 ; Habib & AbouGhaly, 2016 ). For each final model, a valid lack of fit test was censured by a four df pure error and a minimum of three df for lack of fit (Pat & Wayne, 2014 ).…”

Section: Resultsmentioning

confidence: 99%

“…A steep slope or curvature in a line indicates a relatively high sensitivity of response to that MixC. As a result of the effects of different MixCs on each response, contour plots were plotted representing lines of equal response over the design space (Habib & AbouGhaly, 2016 ).…”

Section: Resultsmentioning

confidence: 99%

“…A regression polynomial equation is usually elucidated to represent how the MixCs affect each studied dependent variable (response). The most frequently used models for a three component mixture design are (Habib & AbouGhaly, 2016 ): where is a certain predicted response, the β i , β ij , and β 123 are the coefficients representing, respectively, the linear, quadratic, and special-cubic blending properties of the three MixCs ( x i ).…”

Section: Theoretical Developmentmentioning

confidence: 99%

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D-optimal mixture design for optimization of topical dapsone niosomes: in vitro characterization and in vivo activity against Cutibacterium acnes

2022

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This study aimed to illustrate the use of D-optimal mixture design (DOMD) for optimization of an enhancer containing Dapsone niosomal formula for acne topical treatment. Mixture components (MixCs) studied were: Span 20, Cholesterol, and Cremophor RH. Different responses were measured. Optimized formula (OF) was selected to minimize particle size and maximize absolute zeta potential and entrapment efficiency. Optimized formula gel (OF-gel) was prepared and characterized. OF-gel in vivo skin penetration using confocal laser scanning microscopy and activity against Cutibacterium acnes in acne mouse model were studied. Based on DOMD results analysis, adequate models were derived. Piepel and contour plots were plotted accordingly to explain how alteration in MixCs L-pseudo values affected studied responses and regions for different responses’ values. The OF had suitable predicted responses which were in good correlation with the actually measured ones. The OF-gel showed suitable characterization and in vivo skin penetration up to the dermis layer. In vivo acne mouse-model showed that OF-gel-treated group (OF-gel-T-gp) had significantly better recovery (healing) criteria than untreated (UT-gp) and Aknemycin ® -treated (A-T-gp) groups. This was evident in significantly higher reduction of inflammation percent observed in OF-gel-T-gp than both UT-gp and A-T-gp. Better healing in OF-gel-T-gp compared with other groups was also verified by histopathological examination. Moreover, OF-gel-T-gp and A-T-gp bacterial loads were non-significantly different from each other but significantly lower than UT-gp. Thus, DOMD was an adequate statistical tool for optimization of an appropriate enhancer containing Dapsone niosomal formula that proved to be promising for topical treatment of acne.

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“…d m ranges from 0 to 1. where D is the desirability of the formula ranging from 0 to 1, d m is the individual desirability of each response, m is the number of responses to be optimized (Habib & AbouGhaly, 2016 ).…”

Section: Methodsmentioning

confidence: 99%

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

et al. 2021

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Febuxostat (FXS) is a potent antigout drug with poor water solubility and relative high first-pass effect leading to moderate oral bioavailability (<49%). This study aimed to increase FXS solubility and bioavailability by optimizing sublingual fast-dissolving films (SFs) containing a selected FXS self-nanoemulsifying system (s-SNES) previously prepared by our team. The s-SNES was loaded into SFs by solvent casting technique. A full factorial design (3 2 ) was applied to study the effects of polymer and plasticizer types on mechanical characteristics and the dissolution profile of FXS from the SFs. Numerical optimization was performed to select the SF having highest desirability according to predetermined characteristics. The optimized SF (O-SF) contained 1 g of s-SNES, polyvinylpyrrolidone K30 (6%w/v), polyethylene glycol 300 (20%w/w of polymer wt.), and Avicel PH101 (0.5%w/v). O-SF showed good permeation of FXS through sheep sublingual tissue. Storage of O-SF for three months showed no significant change in the FXS dissolution profile. In-vivo performance of O-SF in rabbits was compared to that of oral marketed tablets (Staturic V R 80 mg). A cross-over design was applied and pharmacokinetic parameters were calculated after ensuring absence of sequence effect. Statistical analysis revealed better performance for O-SF with significantly higher C max , AUC 0-24 , AUC 0-1 , apparent t 1/2 together with lower t max , and apparent k el than marketed tablets. Relative bioavailability of O-SF compared to the marketed tablet was found to be 240.6%. This confirms the achievement of the study aims of improving dissolution rate and bioavailability of FXS using a patient-wise convenient formula.

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Combined mixture-process variable approach: a suitable statistical tool for nanovesicular systems optimization

Abstract: This indicates the validity of combined MPV design and modeling for optimization of transfersomal formulations as an example of nanovesicular systems.

Cited by 22 publications

References 48 publications

Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization

Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization

D-optimal mixture design for optimization of topical dapsone niosomes: in vitro characterization and in vivo activity against Cutibacterium acnes

Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films

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