Solubilization and Release of a Model Drug Nimesulide from PEO–PPO–PEO Block Copolymer Core–Shell Micelles: Effect of Size of PEO Blocks

Parmar, Arpan; Parekh, Paresh; Bahadur, Pratap

doi:10.1007/s10953-012-9949-6

Cited by 17 publications

(6 citation statements)

References 71 publications

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“…The saturation solubility of lyophilized LCDP polymeric micelles was approximately 450 times that of raw LCDP and 300 times that of lyophilized LCDP suspension in both water and 0.1 M HCl. This enhancement in LCDP solubility can be attributed to the interaction between the drug and Pluronic molecules and to the greater number of micelles formed at higher Pluronic to drug ratio (Parmar et al., 2013 ). LCDP solubilization increases by increasing the P123 percentage due to the higher LCDP affinity to the hydrophobic Pluronic (Wei et al., 2009 ).…”

Section: Resultsmentioning

confidence: 99%

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

2017

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This study aims at preparing and optimizing lacidipine (LCDP) polymeric micelles using thin film hydration technique in order to overcome LCDP solubility-limited oral bioavailability. A two-factor three-level central composite face-centered design (CCFD) was employed to optimize the formulation variables to obtain LCDP polymeric micelles of high entrapment efficiency and small and uniform particle size (PS). Formulation variables were: Pluronic to drug ratio (A) and Pluronic P123 percentage (B). LCDP polymeric micelles were assessed for entrapment efficiency (EE%), PS and polydispersity index (PDI). The formula with the highest desirability (0.959) was chosen as the optimized formula. The values of the formulation variables (A and B) in the optimized polymeric micelles formula were 45% and 80%, respectively. Optimum LCDP polymeric micelles had entrapment efficiency of 99.23%, PS of 21.08 nm and PDI of 0.11. Optimum LCDP polymeric micelles formula was physically characterized using transmission electron microscopy. LCDP polymeric micelles showed saturation solubility approximately 450 times that of raw LCDP in addition to significantly enhanced dissolution rate. Bioavailability study of optimum LCDP polymeric micelles formula in rabbits revealed a 6.85-fold increase in LCDP bioavailability compared to LCDP oral suspension.

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Section: Resultsmentioning

confidence: 99%

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

2017

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“…The difference in the spectral behavior of AlPcCl incorporated in P‐123 compared to F‐127 is attributed to the polarity difference of micelles. The copolymer P‐123 is more hydrophobic than F‐127 and has more hydrophobic sites adequate to the PS .…”

Section: Resultsmentioning

confidence: 99%

Formulation of Aluminum Chloride Phthalocyanine in Pluronic^™ P‐123 and F‐127 Block Copolymer Micelles: Photophysical properties and Photodynamic Inactivation of Microorganisms

Vilsinski

Gerola

Enumo

et al. 2015

Photochem & Photobiology

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Aluminum Chloride Phthalocyanine (AlPcCl) can be used as a photosensitizer (PS) for Photodynamic Inactivation of Microorganisms (PDI). The AlPcCl showed favorable characteristics for PDI due to high quantum yield of singlet oxygen (ΦΔ ) and photostability. Physicochemical properties and photodynamic inactivation of AlPcCl incorporated in polymeric micelles of tri-block copolymer (P-123 and F-127) against microorganisms Staphylococcus aureus, Escherichia coli and Candida albicans were investigated in this work. Previously, it was observed that the AlPcCl undergoes self-aggregation in F-127, while in P-123 the PS is in a monomeric form suitable for PDI. Due to the self-aggregation of AlPcCl in F-127, this formulation did not show any effect on these microorganisms. On the other hand, AlPcCl formulated in P-123 was effective against S. aureus and C. albicans and the death of microorganisms was dependent on the PS concentration and illumination time. Additionally, it was found that the values of PS concentration and illumination time to eradicate 90% of the initial population of microorganisms (IC90 and D90 , respectively) were small for the AlPcCl in P-123, showing the effectiveness of this formulation for PDI.

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“…The hydrophobic pluronic L81 (HLB-2) dominated its property in mixed pluronic in the change of size. There are dynamic light scattering reports on pluronic surfactant [ 41–48 ]. Sodium chloride addition, however, showed shrinking in micellar size to 375.7 nm from 413.5 nm which infers that there is no enhancement of drug encapsulation.…”

Section: Resultsmentioning

confidence: 99%

“…Table 2 displays the data of partition coefficients and the Gibb’s free energy of micellization in three systems viz. hydrophilic pluronic F108–water, hydrophobic pluronic L81–water, and mixed pluronic–water [ 41 , 53 ]. As can be noticed, the value of partition coefficient is 1.14 for the pluronic mixture which is higher than that for neat pluronic F108 (1.13) or neat pluronic L81 (0.64).…”

Section: Resultsmentioning

confidence: 99%

Aceclofenac-loaded pluronic F108/L81 mixed polymeric micelles: effect of HLB on solubilization

Senthilkumar

Dash

et al. 2022

Designed Monomers and Polymers

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Pluronic block copolymers have phase behavioural characteristics which are extensively studied for drug delivery applications. In this study, we explored hydrophilic pluronic F108 (HLB = 27), hydrophobic pluronic L81 (HLB = 2) and their mixed micelles acting as solubilising mediums for model drug aceclofenac. The drug solubilisation and interactions have been analysed using UV-visible spectroscopy, Fluorescence spectroscopy, Rheology studies, Fourier-transform infrared spectroscopy, Scanning electron microscope, Dynamic light scattering, Cloud point and partition coefficient measurements. The investigation from UV-spectrophotometry demonstrated that mixed pluronic entrapped greater number of aceclofenac molecules than both the neat pluronics at same concentration. Excimer formation was evidenced from fluorescence spectra with pyrene as a probe. The rheological studies showed difference in viscosity over low shear range. Studies on FTIR demonstrated probable bonding between the aceclofenac and mixed pluronic molecules. The DLS studies on mixed pluronic showed swelling of micellar diameter from 317.6 nm to 413.5 nm. Thermodynamic parameters of the above system revealed higher partition coefficient value for mixed pluronic and spontaneity in drug solubilisation. This study can be exploited to use a hydrophobic copolymeric micelle in mixed pluronic formulation for better drug solubilisation.

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Solubilization and Release of a Model Drug Nimesulide from PEO–PPO–PEO Block Copolymer Core–Shell Micelles: Effect of Size of PEO Blocks

Cited by 17 publications

References 71 publications

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

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

Formulation of Aluminum Chloride Phthalocyanine in Pluronic^™ P‐123 and F‐127 Block Copolymer Micelles: Photophysical properties and Photodynamic Inactivation of Microorganisms

Aceclofenac-loaded pluronic F108/L81 mixed polymeric micelles: effect of HLB on solubilization

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Solubilization and Release of a Model Drug Nimesulide from PEO–PPO–PEO Block Copolymer Core–Shell Micelles: Effect of Size of PEO Blocks

Cited by 17 publications

References 71 publications

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

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

Formulation of Aluminum Chloride Phthalocyanine in Pluronic™ P‐123 and F‐127 Block Copolymer Micelles: Photophysical properties and Photodynamic Inactivation of Microorganisms

Aceclofenac-loaded pluronic F108/L81 mixed polymeric micelles: effect of HLB on solubilization

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Formulation of Aluminum Chloride Phthalocyanine in Pluronic^™ P‐123 and F‐127 Block Copolymer Micelles: Photophysical properties and Photodynamic Inactivation of Microorganisms