Enhancement of dissolution and oral bioavailability of lacidipine via pluronic P123/F127 mixed polymeric micelles: formulation, optimization using central composite design and <i>in vivo</i> bioavailability study

Fares, Ahmed R.; ElMeshad, Aliaa Nabil; Kassem, Mohamed A.

doi:10.1080/10717544.2017.1419512

Cited by 82 publications

(57 citation statements)

References 39 publications

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“…These results differ from the previous research results that a decrease in the properties of hydrophilicity in a copolymer triblock can increase the particle size [11]. However, it is expressed in other studies that the greater the molecular weight of the PEG in the PECE triblock copolymer can provide a stabilization effect of the colloidal steric on its hydrophiles so that with a low PEG composition can lower the particle size [6,12]. Graphic influence ratio of PCL/PEG on particle size can be seen in fig.…”

Section: Particle Sizecontrasting

confidence: 90%

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Optimization and Characterization of Peg-PCL-Peg Triblock Copolymer as Carrier of Drug Using Full Factorial Design

Armatazaka

Sulaiman²,

Zulkarnain

2019

Int J Curr Pharm Sci

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Objective: Triblock copolymer of poly(ethylene glycol)-poly(ɛ-caprolactone)-poly(ethylene glycol) (PEG-PCL-PEG, PECE) was applicated as hydrophobic drug. This study aims to optimization and characterization of PECE triblock copolymer as carriers of hydrophobic drug (ketoprofen).Methods: Triblock copolymer of PECE was prepared with varying composition ratio of PEG and PCL by ring-opening and coupling reaction. The characteristics of triblock copolymer were characterized using FTIR and DSC. Variation composition ratio of poly(ɛ-caprolactone) (PCL)/poly(ethylene glycol) (PEG) and ratio PECE/drug as factors for optimization using full factorial design. Ketoprofen was loaded into PECE triblock copolymer micelles by emulsification and solvent evaporation method. Responses were measured particle size, entrapment efficiency (EE) and drug solubility. Results:The result of this study showed that a higher ratio of PCL/PEG and ratio of PECE/drug, reducing particle size, increasing EE and improving drug solubility. The optimum formula obtained by ratio of PCL/PEG is 2:1 and ratio of PECE/drug is 40:1 with particle size is 356,967±9,142 nm, EE is 57,751±0,437%, drug solubility is 32,648±0,200 µg/ml and zeta potential-18,867±2,578 mV. A full factorial design was applied to determine the optimum formula for the PECE triblock copolymer as drug carriers. Conclusion:The PECE triblock copolymer was preparated using ring-opening polymerization method with Sn(Oct)2 as a catalyst and then continued the reaction with HMDI as coupling agent. Ketoprofen was loaded into PECE triblock copolymer using methods emulsification and solvent evaporation.

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Section: Particle Sizecontrasting

confidence: 90%

“…The factors used are the ratio of PCL/PEG (X1) and ratio of PECE/drugs (X2). Tests used in response include particle size (Y1), entrapment efficiency (EE) (Y2) and drug solubility (Y3) (table 1) [6,7].…”

Section: Fig 1: Schematic Formation Of the Pece Triblock Copolymermentioning

confidence: 99%

Optimization and Characterization of Peg-PCL-Peg Triblock Copolymer as Carrier of Drug Using Full Factorial Design

Armatazaka

Sulaiman²,

Zulkarnain

2019

Int J Curr Pharm Sci

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“…Nanomicellar loading with therapeutics and imaging tools such as fluorescence Rhodamine and FITC probes are used for drug released imaging at specific tumour sites with distinctive designed image. Hence, nanomicelles are favourable as carriers for combinational chemotherapeutics and nanodiagnostic tools [98][99][100].…”

Section: Diagnosis Of Ovarian Cancer Employing Nanomicellesmentioning

confidence: 99%

Nanodrug Delivery Systems for the Treatment of Ovarian Cancer

Pantshwa

Kondiah

Choonara

et al. 2020

Cancers

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Despite advances achieved in medicine, chemotherapeutics still has detrimental side effects with ovarian cancer (OC), accounting for numerous deaths among females. The provision of safe, early detection and active treatment of OC remains a challenge, in spite of improvements in new antineoplastic discovery. Nanosystems have shown remarkable progress with impact in diagnosis and chemotherapy of various cancers, due to their ideal size; improved drug encapsulation within its interior core; potential to minimize drug degradation; improve in vivo drug release kinetics; and prolong blood circulation times. However, nanodrug delivery systems have few limitations regarding its accuracy of tumour targeting and the ability to provide sustained drug release. Hence, a cogent and strategic approach has focused on nanosystem functionalization with antibody-based ligands to selectively enhance cellular uptake of antineoplastics. Antibody functionalized nanosystems are (advanced) synthetic candidates, with a broad range of efficiency in specific tumour targeting, whilst leaving normal cells unaffected. This article comprehensively reviews the present status of nanosystems, with particular emphasis on nanomicelles for molecular diagnosis and treatment of OC. In addition, biomarkers of nanosystems provide important prospects as chemotherapeutic strategies to upsurge the survival rate of patients with OC.

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“…Some papers are present in the literature using DoE in the development of nanomedicines [21] and more specifically of polymeric micelles. Some of them refer to systems based on poloxamers [22,23], and in a few cases, HA-based polymeric micelles have been developed [24]. In the present work, in a first phase, a screening full factorial design 2 3 was used, and as response (dependent) variables, nanoparticles' dimensions and CLO concentration in final colloidal dispersion were considered.…”

Section: Introductionmentioning

confidence: 99%

Design of Experiments-Assisted Development of Clotrimazole-Loaded Ionic Polymeric Micelles Based on Hyaluronic Acid

et al. 2020

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Polymeric micelles based on amphiphilic polysaccharides have some advantages as a carrier of poorly soluble lipophilic drugs thanks to their characteristic "core–shell" structure. Previously, ionic polymeric micelles based on chitosan and fatty acids have been developed. The aim of the present study was the preparation and characterization of hyaluronic acid (HA) derivatives by direct ionic interaction between the HA carboxylic groups and the amine groups of dodecyl amine (DDA) and hexadecyl amine (HDA). The HA–HDA polymeric micelles were loaded with a poorly soluble hydrophobic antifungal drug, clotrimazole (CLO). A 23 full factorial experimental design was used to evaluate the effect of the following factors: HA/HDA ratio from 1:0.25 to 1:0.75, cholesterol (CHOL%) as percentage of HA from 10% to 30%, and preparation temperature from 20 to 40 °C. As dependent variables (responses), nanoparticle dimensions and clotrimazole concentration in the final colloidal dispersion were considered. To optimize the drug final concentration, the design was therefore expanded into a rotatable central composite design (CCD). The effects of the formulation variables and the composition of the optimized formulation were confirmed by a mixture design. Physicochemical characterization of the optimized formulation was performed, confirming the ionic interaction between the polysaccharide and the HDA.

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Enhancement of dissolution and oral bioavailability of lacidipine via pluronic P123/F127 mixed polymeric micelles: formulation, optimization using central composite design and in vivo bioavailability study

Cited by 82 publications

References 39 publications

Optimization and Characterization of Peg-PCL-Peg Triblock Copolymer as Carrier of Drug Using Full Factorial Design

Optimization and Characterization of Peg-PCL-Peg Triblock Copolymer as Carrier of Drug Using Full Factorial Design

Nanodrug Delivery Systems for the Treatment of Ovarian Cancer

Design of Experiments-Assisted Development of Clotrimazole-Loaded Ionic Polymeric Micelles Based on Hyaluronic Acid

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