Application of multiple response optimization technique to extended release formulations design

Hamed, Ehab; Sakr, Adel

doi:10.1016/s0168-3659(01)00356-x

Cited by 107 publications

(35 citation statements)

References 15 publications

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“…The α value is defined as the distance of the axial runs from the center of the design and equals the fourth root of the number of factorial runs ((2 2 ) 1/4 = 1.414). 37 The amounts of LTG and deionized water (pH 7.4) were selected as the factors, and studied at five levels each. The central point (0, 0) was studied five times.…”

Section: Optimization Of P123/ltg Micelles Through Ccd/response Surfamentioning

confidence: 99%

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Liu¹,

Wang²,

Zhou³

et al. 2014

IJN

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Background P-glycoprotein (P-gp) mediated drug efflux across the blood–brain barrier (BBB) is an important mechanism underlying poor brain penetration of certain antiepileptic drugs (AEDs). Nanomaterials, as drug carriers, can overcome P-gp activity and improve the targeted delivery of AEDs. However, their applications in the delivery of AEDs have not been adequately investigated. The objective of this study was to develop a nano-scale delivery system to improve the solubility and brain penetration of the antiepileptic drug lamotrigine (LTG). Methods LTG-loaded Pluronic ® P123 (P123) polymeric micelles (P123/LTG) were prepared by thin-film hydration, and brain penetration capability of the nanocarrier was evaluated. Results The mean encapsulating efficiency for the optimized formulation was 98.07%; drug-loading was 5.63%, and particle size was 18.73 nm. The solubility of LTG in P123/LTG can increase to 2.17 mg/mL, making it available as a solution. The in vitro release of LTG from P123LTG presented a sustained-release property. Compared with free LTG, the LTG-incorporated micelles accumulated more in the brain at 0.5, 1, and 4 hours after intravenous administration in rats. Pretreatment with systemic verapamil increased the rapid brain penetration of free LTG but not P123/LTG. Incorporating another P-gp substrate (Rhodamine 123) into P123 micelles also showed higher efficiency in penetrating the BBB in vitro and in vivo. Conclusion These results indicated that P123 micelles have the potential to overcome the activity of P-gp expressed on the BBB and therefore show potential for the targeted delivery of AEDs. Future studies are necessary to further evaluate the appropriateness of the nanocarrier to enhance the efficacy of AEDs.

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Section: Optimization Of P123/ltg Micelles Through Ccd/response Surfamentioning

confidence: 99%

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Liu¹,

Wang²,

Zhou³

et al. 2014

IJN

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“…The model independent approaches ANOVA-based methods [3,13] and similarity criteria for heterocedasticy, absent in previous approaches. based on various indexes for pairwise comparison Also introduced was an additional parameter to procedures [14][15][16][17][18][19]. It should also be pointed out describe the asymptotic value of the dissolution that some of the methods rely on the individual profile.…”

Section: Introductionmentioning

confidence: 99%

Comparison of dissolution profiles of Ibuprofen pellets

Costa

Sousa

Pais

et al. 2003

Journal of Controlled Release

148

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In this work we use both model dependent and independent techniques to assess the difference between dissolution profiles in which ibuprofen, in the form of uncoated pellets, is used as a model drug. The choice of a proper regression function, the relevance of the estimated parameters and the influence of the choice of dissolution points in the assessment of differences is discussed. The results obtained via mean dissolution times (MDT) and fit-factors ( f and f ) are also discussed 1 2and a non-quantitative method based on profiles correlation with graphical representation (concentration vs. concentration and rate vs. rate) presented. The tested methods discriminate similarly between curves, although not in all cases, but those based on modeling, MDT and fit-factors have shown to be less informative than the correlation approach. 

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“…Planning pharmaceutical formulation with the least of trial is very challenging for pharmaceutical researchers [20]. In conventional optimization method, a single factor is varied meanwhile the other factors are fixed at a particular set of settings.…”

Section: Formulation Optimization By Central Composite Designmentioning

confidence: 99%

Development of Alginate–Gum Arabic Beads for Targeted Delivery of Protein

Mohamed¹,

Mustafa²,

Fitrianto³

et al. 2017

J Biomol Res Ther

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Controlled release beads were prepared by using the combination of alginate and gum Arabic through ionotropic gelation method. Bovine serum albumin was used as model protein for in vitro assessments. The effect of amount of sodium alginate and gum Arabic as the factor affecting protein encapsulation efficiency and protein release were optimized and analyzed by using RSM-FCCD. It was observed that protein encapsulation efficiency was increased and protein release was decreased with the increase of both of the amount of sodium alginate and gum Arabic, used as polymer blend. The optimized beads showed high encapsulation efficiency (87.5 ± 3.65%) with suitable protein release (100% protein release after almost 4 hrs). The swelling of beads were highly influenced by pH of dissolution medium. These beads were also characterized by FT-IR spectroscopy, SEM and TA for protein-excipients interaction, beads surface morphology and beads strength, respectively. These calcium alginate/gum Arabic beads have good potential to be used as delivery vehicle for protein drugs.

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Application of multiple response optimization technique to extended release formulations design

Cited by 107 publications

References 15 publications

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Comparison of dissolution profiles of Ibuprofen pellets

Development of Alginate–Gum Arabic Beads for Targeted Delivery of Protein

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Application of multiple response optimization technique to extended release formulations design

Cited by 107 publications

References 15 publications

Enhanced brain delivery of lamotrigine with Pluronic&reg; P123-based nanocarrier

Enhanced brain delivery of lamotrigine with Pluronic&reg; P123-based nanocarrier

Comparison of dissolution profiles of Ibuprofen pellets

Development of Alginate–Gum Arabic Beads for Targeted Delivery of Protein

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Product

Resources

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Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier