Formulation and in vitro evaluation of polymeric enteric nanoparticles as dermal carriers with pH-dependent targeting potential

Sahle, Fitsum Feleke; Balzus, Benjamin; Gerecke, Christian; Kleuser, Burkhard; Bodmeier, Roland

doi:10.1016/j.ejps.2016.07.004

Cited by 47 publications

(15 citation statements)

References 31 publications

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“…Nanoparticle approaches like polymeric nanoparticles have been found promising to overcome traditional problems as low solubility, higher stability, sharper size distribution, sustained and controlled release profiles, higher encapsulation efficiency for weakly water soluble agents and can be effective in enhancing bioavailability with better targeting efficiency [ 15 , 16 ]. Chitosan found to carry a variety of hydrophilic and hydrophobic drugs and poloxamer 407 is a nonionic US FDA approved stabilizer used in various formulations [ 17 , 18 , 19 ]. However, the surface properties of polymeric nanoparticles are altered by surface modification and/or to improve the pharmacokinetics of these colloidal carriers here chitosan is used as a polymer [ 16 , 20 ].…”

Section: Introductionmentioning

confidence: 99%

Chitosan and glyceryl monooleate nanostructures containing gallic acid isolated from amla fruit: targeted delivery system

Patil

Killedar²

2021

Heliyon

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Gallic acid, active constituent of amla fruit its natural abundance with beneficial multi actions in body make them attractive for clinical applications. In present study, we focused on extracting, separating and characterizing gallic acid from amla and further formulated into chitosan nanoparticles, so bring it to increase its aqueous solubility and thereby bioactivity. Gallic acid nanoparticles were prepared by using poloxamer 407, chitosan and Glyceryl Monooleate (GMO) using probe sonicator and high pressure homogenization method. Prepared nanoparticles were characterized by particle size, zeta potential, DSC, XRD, SEM, entrapment efficiency, loading content, in-vitro release and stability study. They showed approximately 76.80% encapsulation of gallic acid with average size of 180.8 ± 0.21 nm, and zeta potential + 24.2 mV. The cumulative in vitro drug release upto 24 hrs 77.16% was achieved suggesting that from all our findings, it can be concluded that work will facilitate extraction, design and fabrication of nanoparticles for protection and sustained release of gallic acid particularly to colonic region.

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Section: Introductionmentioning

confidence: 99%

Chitosan and glyceryl monooleate nanostructures containing gallic acid isolated from amla fruit: targeted delivery system

Patil

Killedar²

2021

Heliyon

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“…Franz chambers, a popular method for measuring the diffusion rates, were used to determine substance permeation released from the carrier through a membrane imitating artificial skin in a PBS environment [29]. The Franz diffusion cell test enabled the in vitro evaluation of polymeric enteric nanoparticles as the dermal carriers with pH-dependent targeting potential [30], or the assessment of the reverse micelle of lipophile-functionalized PEG dendrimer hybrids for applications in carrier-mediated transdermal drug delivery [31]. Therefore, Franz diffusion cells were also selected to evaluate the permeation through the membrane of the studied micellar carriers and conjugates.…”

Section: Permeation Testsmentioning

confidence: 99%

PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery

2020

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The in vitro biochemical evaluation of the applicability of polymers carrying active substances (micelles and conjugates) was carried out. Previously designed amphiphilic graft copolymers with retinol or 4-n-butylresorcinol functionalized polymethacrylate backbone and poly(ethylene glycol) (PEG) side chains that included Janus-type heterografted copolymers containing both PEG and poly(ε-caprolactone) (PCL) side chains were applied as micellar carriers. The polymer self-assemblies were convenient to encapsulate arbutin (ARB) as the selected active substances. Moreover, the conjugates of PEG graft copolymers with ferulic acid (FA) or lipoic acid (LA) were also investigated. The permeability of released active substances through a membrane mimicking skin was evaluated by conducting transdermal tests in Franz diffusion cells. The biological response to new carriers with active substances was tested across cell lines, including normal human dermal fibroblasts (NHDF), human epidermal keratinocyte (HaCaT), as well as cancer melanoma (Me45) and metastatic human melanoma (451-Lu), for comparison. These polymer systems were safe and non-cytotoxic at the tested concentrations for healthy skin cell lines according to the MTT test. Cytometric evaluation of cell cycles as well as cell death defined by Annexin-V apoptosis assays and senescence tests showed no significant changes under action of the delivery systems, as compared to the control cells. In vitro tests confirmed the biochemical potential of these antioxidant carriers as beneficial components in cosmetic products, especially applied in the form of masks and eye pads.

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“…Polymethylmethacrylate (PMMA) polymers (Eudragit) are employed as drug delivery systems targeting different specific organs such as stomach, duodenum and colon, epithelial cells and their membranes, skin surface, and hair follicles …”

Section: Introductionmentioning

confidence: 99%

Effect of secondary polymer on self‐precipitation of pH‐sensitive polymethylmethacrylate derivatives Eudragit E100 and Eudragit L100

Ofridam

Lebaz

Gagnière

et al. 2020

Polymers for Advanced Techs

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Interpolyelectrolyte complexes or polyplexes can be seen as interesting alternatives in the purpose of active ingredients encapsulation. Working on polymethylmethacrylate derivatives with special focus on controlled oral drug delivery, the influence of charged polyelectrolytes (polyacrylic acid, polyethylenimine, and aminodextran) and noncharged ones (polyvinyl alcohol, dextran 40, and Pluronic F68) has been investigated on the precipitation of two pH-sensitive Eudragit polymers, namely, L100 and E100. Moreover, the possibility of preparing polyplexes involving the two polymethylmethacrylate derivatives with different charged and noncharged secondary polyelectrolytes has been studied. The obtained dispersions have been characterized in terms of mean particle size, size distribution, zeta potential, and morphology. Direct precipitation of Eudragit L100 by medium acidification in a batch process and in the presence of polyethylenimine allowed the production of particles with a narrow size distribution. The mean size was around 200 nm. In this case, the zeta potential was found to be +45 mV at pH = 7 in 1mM aqueous NaCl solution, and the produced suspension was stable in time since no aggregation and sedimentation have been observed. A precipitation pH of 8.16 allows us to suggest the preparation of a polyplex based on Eudragit L100 and polyethylenimine. In contrary, polyvinyl alcohol has shown ability to induce an increase in particle mean size whereas other polyelectrolytes showed no significant effect. Moreover, it was observed that polyethylenimine and polyacrylic acid solutions were able to directly induce Eudragit E100 precipitation whereas amino-dextran and noncharged polyelectrolytes showed no effect on its precipitation and on particle size distribution. K E Y W O R D S dispersion, pH-sensitive polymers, polyplex, precipitation, self-precipitation 1 | INTRODUCTION Several polymers are nowadays used for the encapsulation of active molecules. This process covers a broad range of applications such as pharmaceutical, food, cosmetic, and textile industries. Among the commonly used coating materials, biodegradable polymers such as polysaccharides (starch and chitosan), proteins (gelatin and bovine serum albumin), polyesters (polylactide [PLA], polylactide-co-glycolide [PLGA], and polycaprolactone [PCL]), and polyether (polyethylene glycol [PEG]) are explored in the literature. 1 Moreover, nonbiodegradable stimuli-responsive polymers are largely studied especially the polymethylmethacrylate derivatives. 2

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Formulation and in vitro evaluation of polymeric enteric nanoparticles as dermal carriers with pH-dependent targeting potential

Cited by 47 publications

References 31 publications

Chitosan and glyceryl monooleate nanostructures containing gallic acid isolated from amla fruit: targeted delivery system

Chitosan and glyceryl monooleate nanostructures containing gallic acid isolated from amla fruit: targeted delivery system

PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery

Effect of secondary polymer on self‐precipitation of pH‐sensitive polymethylmethacrylate derivatives Eudragit E100 and Eudragit L100

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