Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Elzoghby, Ahmed O.; Helmy, Maged W.; Samy, Wael M.; Elgindy, Nazik A.

doi:10.2147/ijn.s40674

Cited by 95 publications

(37 citation statements)

References 37 publications

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“…2 The proteins are considered ideal for drug delivery applications due to their exceptional properties, e.g., biodegradability, biocompatibility, low toxicity, abundant renewable sources, ease of scaling up during manufacturing, and their being metabolizable. 2,3 Common examples include albumin, collagen, gelatin, whey protein, and casein. 4−6 Food proteins are of particular interest due to their high nutritional value and outstanding functional features, namely emulsification, gelation, water binding and foaming ability, and their application in the food industry.…”

Section: ■ Introductionmentioning

confidence: 99%

Celecoxib Encapsulation in β-Casein Micelles: Structure, Interactions, and Conformation

et al. 2015

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β-Casein is a 24 kDa natural protein that has an open conformation and almost no folded or secondary structure, and thus is classified as an intrinsically unstructured protein. At neutral pH, β-casein has an amphiphilic character. Therefore, in contrast to most unstructured proteins that remain monomeric in solution, β-casein self-assembles into well-defined core-shell micelles. We recently developed these micelles as potential carriers for oral administration of poorly water-soluble pharmaceuticals, using celecoxib as a model drug. Herein we present deep and precise insight into the physicochemical characteristics of the protein-drug formulation, both in bulk solution and in dry form, emphasizing drug conformation, packing properties and aggregation state. In addition, the formulation is extensively studied in terms of structure and morphology, protein/drug interactions and physical stability. Particularly, NMR measurements indicated strong drug-protein interactions and noncrystalline drug conformation, which is expected to improve drug solubility and bioavailability. Small-angle X-ray scattering (SAXS) and cryogenic transmission electron microscopy (cryo-TEM) were combined for nanostructural characterization, proving that drug-protein interactions lead to well-defined spheroidal micelles that become puffier and denser upon drug loading. Dynamice light scattering (DLS), turbidity measurements, and visual observations complemented the analysis for determining formulation structure, interactions, and stability. Additionally, it was shown that the loaded micelles retain their properties through freeze-drying and rehydration, providing long-term physical and chemical stability. Altogether, the formulation seems greatly promising for oral drug delivery.

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Section: ■ Introductionmentioning

confidence: 99%

Celecoxib Encapsulation in β-Casein Micelles: Structure, Interactions, and Conformation

et al. 2015

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“…Concentration of flutamide present in the supernatant was determined by UV spectrophotometer at 228 nm [13].…”

Section: Drug Contentmentioning

confidence: 99%

Design and Evaluation of Flutamide-Loaded Polycaprolactone Nanoparticles by 23 Factorial Design and Nanoprecipitation Method

2018

Asian J Pharm Clin Res

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Objective: The present work was aimed to prepare and evaluate polymeric nanoparticles (NPs) of flutamide by nanoprecipitation method and factorial. The influences of various formulation components such as polymer, organic phase volume, and surfactant on the characteristics of NPs were investigated.Methods: The polycaprolactone (PCL) loaded with drug was evaluated for surface morphology, surface charge, particles size, encapsulation efficiency, drug content, and in vitro release studies. Fourier transform infrared studies were indicated no interaction between the drug and polymer.Results: The results of the drug release study of NPs may fit with different kinetic equations. The particle size varied from 128 to 317 nm and zeta potential was in negative and its value found to be - 46.4 mv. The content of flutamide was found in between 74%±0.72 to 92%±0.53 in flutamide loaded PCL NPs. The minimum and maximum entrapment efficiencies were found to be of 75%±0.66 and 92%±0.70. The percentage yields of all formulations were in the range of 46.05%±1.56–86.78%±1.32. The in vitro drug release followed zero order with sustained behavior for a period of 24 h. Results of accelerated storage conditions of optimized formulation revealed that no significant changes in formulation F2.Conclusion: The present investigation opens new frontiers in developing flutamide NPs for targeting delivery to the prostate for the prostate cancer treatment which also overcome the problems associated with conventional formulations such as multiple-dose therapy, poor patient compliance, and high treatment cost.

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“…Zein NPs have been prepared by pH controlled nanoprecipitation method (Satheesh and Omathanu 2010). While casein NPs have been prepared by ionotropic gelation method using TPP as cross-linker (Elzoghby et al 2013). …”

Section: Synthesis Of Protein Nanoparticlesmentioning

confidence: 99%

Biodegradable Nanoparticles and Their In Vivo Fate

Kumari

Singla

Guliani

et al. 2016

Nanoscale Materials in Targeted Drug Delivery, Theragnosis and Tissue Regeneration

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Biodegradable nanoparticles (BNPs) are seeking augmented attention for their ability to serve as a carrier for site-specific delivery of drugs, biomolecules, proteins and peptides in the body. They offer enhanced biocompatibility, better drug encapsulation and sustained release profile of a great number of drugs and biomolecules to be used in a variety of applications in nanomedicine. The use of BNPs for controlled drug delivery has shown significant therapeutic potential. Concurrently, targeted delivery technologies are becoming an increasingly important area of scientific investigation. The fate of BNPs is decided by virtue of their physiochemical properties in biological medium. Another important area which is gaining attention of researchers is the behaviour of BNPs in biological milieu. In the present chapter, efforts are made to give the readers a comprehensive outlook of the topic covering the following major points: (1) brief introduction to BNPs; (2) synthesis methodologies of BNPs; (3) characterisation of BNPs; (4) BNPs for drug delivery; (5) drug release mechanisms from BNPs; (6) targeted drug delivery using BNPs; (7) biological barriers encountered by BNPs; and (8) in vivo fate of BNPs.

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Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Cited by 95 publications

References 37 publications

Celecoxib Encapsulation in β-Casein Micelles: Structure, Interactions, and Conformation

Celecoxib Encapsulation in β-Casein Micelles: Structure, Interactions, and Conformation

Design and Evaluation of Flutamide-Loaded Polycaprolactone Nanoparticles by 23 Factorial Design and Nanoprecipitation Method

Biodegradable Nanoparticles and Their In Vivo Fate

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