ffect of Polymer and Formulation Variables on Properties of Self- Assembled Polymeric Micellar Nanoparticles

Bhambere, Deepak

doi:10.4172/2155-983x.1000129

Cited by 4 publications

(3 citation statements)

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“…53 It could be inferred that higher amounts of the copolymer are available to entrap the loaded drug. Similar findings were reported by Bhambere et al 60 for paclitaxelloaded PLGA nanoparticles, by Kizilbey 61 for rutin-loaded PLGA nanoparticles, by Nahata et al 41 for aripiprazoleloaded PLGA microspheres and by Wagh et al 62 for cyclosporine A-loaded PLGA nanoparticles.…”

Section: Estimation Of Drug Encapsulation Efficiency (Ee%)supporting

confidence: 84%

Eudragit®-S100 Coated PLGA Nanoparticles for Colon Targeting of Etoricoxib: Optimization and Pharmacokinetic Assessments in Healthy Human Volunteers

El-Maghawry¹,

Tadros²,

Elkheshen³

et al. 2020

IJN

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Aim: Etoricoxib is a selective inhibitor of COX-2 enzyme. It is proposed as a potent antiinflammatory drug intended for the control of irritable bowel syndrome. The current work aimed at developing etoricoxib-loaded nanoparticles for colon-targeting. Materials and Methods: PLGA nanoparticles were developed via nano-spray drying technique. The D-optimal design was adopted for the investigation of the influence of i) DL-lactidecoglycolide (PLGA) concentration, ii) polyvinylpyrrolidone K30 (PVP K30) concentration and iii) lactide:glycolide ratio in the copolymer chain on the yield%, the encapsulation efficiency (EE %), particle size (PS) and percentage of drug release after 2h (P 2h ), 4h (P 4h ) and 12h (P 12h ). To promote colon targeting of the systems, the best achieved system (M14) was either directly coated with poly(methacrylic acid-co-methyl methacrylate) [Eudragit ® -S100] or loaded into hard gelatin capsules and the capsules were coated with poly(methacrylic acid-co-methyl methacrylate) (E-M14C). The pharmacokinetic parameters of etoricoxib following oral administration of E-M14C in healthy volunteers were assessed relative to commercial etoricoxib tablets. Results: M14 system was prepared using PLGA (0.5% w/v) at a lactide:glycolide ratio of 100:0, in the presence of PVP K30 (2% w/v). M14 system was nano-spherical particles of 488 nm size possessing promising yield% (63.5%) and EE% (91.2%). The percentage drug released after 2, 4 and 12 hours were 43.41%, 47.34 and 64.96%, respectively. Following M14-loading into hard gelatin capsules and coating with poly(methacrylic acid-co-methyl methacrylate) [Eudragit-S100], the respective P 2h , P 4h and P 12h were 10.1%, 28.60% and 65.45%. Significant (p < 0.05) differences between the pharmacokinetic parameter of E-M14C in comparison with the commercial product were revealed with a delay in T max (from 2.5h to 6h), a prolongation in MRT 0-∞ (from 24.4h to 34.7h) and an increase in the relative oral bioavailability (4.23 folds). Conclusion: E-M14C is a potential system for possible colon targeting of etoricoxib.

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Section: Estimation Of Drug Encapsulation Efficiency (Ee%)supporting

confidence: 84%

Eudragit®-S100 Coated PLGA Nanoparticles for Colon Targeting of Etoricoxib: Optimization and Pharmacokinetic Assessments in Healthy Human Volunteers

El-Maghawry¹,

Tadros²,

Elkheshen³

et al. 2020

IJN

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“…During spray drying inlet and outlet temperature was set at 150 °C and 90 °C respectively. Aspirator rate was adjusted at 35Nm 3 /hr while sample feed rate was 2 ml/min [ 16 ]. With same procedure one batch of PLGA 50:50 was also prepared at optimized condition of PLGA 75:25 and it was also evaluated for same parameters simultaneously along with 75:25 grade nanoparticles.…”

Section: Methodsmentioning

confidence: 99%

Formulation of PPAR-gamma agonist as surface modified PLGA nanoparticles for non-invasive treatment of diabetic retinopathy: in vitro and in vivo evidences

Laddha

Kshirsagar

2020

Heliyon

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Diabetic retinopathy is one of the worst complications of diabetes and it is treated by invasive method. We prepared a surface modified poly (D, L-lactide-co-glycolide) i.e. PLGA nanoparticles for delivery of pioglitazone-a peroxisome proliferator-activated receptor-gamma agonist to posterior segment of the eye by topical administration. The present study investigated two grades of PLGA viz. 75:25 and 50:50. Surface modification was performed using polysorbate 80. Nanoparticles were prepared by single emulsion solvent evaporation method and optimized by using 3-factor 3-level Box-Behnken statistical design. Mean particle size, PDI and entrapment efficiency for optimized batch of PLGA 75:25 was found to be 163.23 nm, 0.286 and 91%, whereas; for PLGA 50:50 it was 171.7 nm, 0.280 and 93% respectively. DSC confirms the molecular dispersion of drug in polymer. In vitro release study showed biphasic drug release pattern with 58.48 ± 1.38% and 74.17 ± 1.38% cumulative drug release by PLGA 75:25 and 50:50 nanoparticles at the end of 10h. The release profile of pioglitazone from nanoparticles appeared to fit best with Higuchi model. In vivo study on rat showed dose dependent reduction in vascular endothelial growth factor concentration in vitreous fluid. The study reveals significance of peroxisome proliferator-activated receptor-gamma in management of diabetic retinopathy.

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“…Thus, by designing a novel delivery system for targeted Erlo delivery, poor solubility, cell selectivity and low bioavailability can be improved [2]. The different encapsulation methods that are used as delivery systems include liposomes, polymeric-based nanoparticles [3,4], hydrogels, and serum albumin. Among the variety of targeting ligands, hyaluronic acid (HA) and human serum albumin have proven success in lung cancer targeting with in tumour cell lines animal models [5].…”

Section: Introductionmentioning

confidence: 99%

Design, Development and in Vitro Evaluation of Erlotinib Loaded Liquorice Crude Protein Nanoparticles by Box Behnken Design

Geetha

Velraj

2021

Int J App Pharm

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Objective: To formulate and evaluate Erlotinib loaded Liquorice crude protein (LCP) nanoparticles from the powdered liquorice root (Glycyrrhiza glabra) using Box-Behnken design. Methods: Erlotinib loaded liquorice crude protein nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) and gluteraldehyde (8% v/v) as cross linking agent. Box-Behnken design with 3 factors, 3 levels and 3 responses was used to optimize the prepared nanoparticles. The independent variables were taken as A) Erlotinib concentration B) LCP concentration and C) Incubation time with responses R1) Drug entrapment efficiency R2) Drug Release and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, and in vitro drug release studies in PBS pH 7.4 (26 h) were carried out. The experimental values were found to be in close resemblance with the predicted value obtained from the optimization process. The in vitro cytotoxicity studies of the prepared nanoparticles in lung cancer cell line (A 549) were studied with different concentrations for 24h. Results: The average particle size, zeta potential, Polydispersity index (PDI) were found to be 292.1 nm,-25.8 mV and 0.384 respectively. TEM image showed that the nanoparticles dispersed well with a uniform shape and showed not much change during storage. The in vitro drug release showed 41.23% for 26 h in PBS (7.4) and release kinetics showed highest R2value (0.982) for Korsmeyer-Peppas model, followed by 0.977 for Higuchi model. The in vitro cytotoxicity of prepared nanoparticles in A 549 cell line showed good results with different concentrations for 24h. Conclusion: Erlotinib (Erlo) is a BCS class II drug with poor solubility, poor bioavailability and selective tyrosine kinase inhibitor for non small-cell lung cancer (NSCLC) through oral administration. To improve the oral bioavailability and absorption of molecules, plant protein as carriers is used for developing drug delivery systems due to their proven safety. The optimization variables were Conc of Erlo, Conc. of LCP and Incubation time to get responses as drug entrapment efficiency, drug release and particle size. The compatibility between drug and LCP were evaluated by FTIR.

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ffect of Polymer and Formulation Variables on Properties of Self- Assembled Polymeric Micellar Nanoparticles

Cited by 4 publications

References 0 publications

<p>Eudragit<sup>®</sup>-S100 Coated PLGA Nanoparticles for Colon Targeting of Etoricoxib: Optimization and Pharmacokinetic Assessments in Healthy Human Volunteers</p>

<p>Eudragit<sup>®</sup>-S100 Coated PLGA Nanoparticles for Colon Targeting of Etoricoxib: Optimization and Pharmacokinetic Assessments in Healthy Human Volunteers</p>

Formulation of PPAR-gamma agonist as surface modified PLGA nanoparticles for non-invasive treatment of diabetic retinopathy: in vitro and in vivo evidences

Design, Development and in Vitro Evaluation of Erlotinib Loaded Liquorice Crude Protein Nanoparticles by Box Behnken Design

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