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In Vitro Bioeffects of Polyelectrolyte Multilayer Microcapsules Post-Loaded with Water-Soluble Cationic Photosensitizer.

ABSTRACT: Microencapsulation and targeted delivery of cytotoxic and antibacterial agents of photodynamic therapy (PDT) improve the treatment outcomes for infectious diseases and cancer. In many cases, the loss of activity, poor encapsulation efficiency, and inadequate drug dosing hamper the success of this strategy. Therefore, the development of novel and reliable microencapsulated drug formulations granting high efficacy is of paramount importance. Here we report the in vitro delivery of a water-soluble cationic PDT drug, zinc phthalocyanine choline derivative (Cholosens), by biodegradable microcapsules assembled from dextran sulfate (DS) and poly-l-arginine (PArg). A photosensitizer was loaded in pre-formed [DS/PArg]4 hollow microcapsules with or without exposure to heat. Loading efficacy and drug release were quantitatively studied depending on the capsule concentration to emphasize the interactions between the DS/PArg multilayer network and Cholosens. The loading data were used to determine the dosage for heated and intact capsules to measure their PDT activity in vitro. The capsules were tested using human cervical adenocarcinoma (HeLa) and normal human dermal fibroblast (NHDF) cell lines, and two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. Our results provide compelling evidence that encapsulated forms of Cholosens are efficient as PDT drugs for both eukaryotic cells and bacteria at specified capsule-to-cell ratios.

SUBMITTER: Ermakov AV

PROVIDER: S-EPMC7408512 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature

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In Vitro Bioeffects of Polyelectrolyte Multilayer Microcapsules Post-Loaded with Water-Soluble Cationic Photosensitizer.

Ermakov Alexey V AV Verkhovskii Roman A RA Babushkina Irina V IV Trushina Daria B DB Inozemtseva Olga A OA Lukyanets Evgeny A EA Ulyanov Vladimir J VJ Gorin Dmitry A DA Belyakov Sergei S Antipina Maria N MN

Pharmaceutics 20200630 7

Microencapsulation and targeted delivery of cytotoxic and antibacterial agents of photodynamic therapy (PDT) improve the treatment outcomes for infectious diseases and cancer. In many cases, the loss of activity, poor encapsulation efficiency, and inadequate drug dosing hamper the success of this strategy. Therefore, the development of novel and reliable microencapsulated drug formulations granting high efficacy is of paramount importance. Here we report the in vitro delivery of a water-soluble ...[more]

PMID: 32629864

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Project description:The field of membranes saw huge developments in the last decades with the introduction of both polyelectrolyte multilayer (PEM)-based membranes and biomimetic membranes. In this work, we combine these two promising systems and demonstrate that proteopolymersomes (PP+) with the incorporated aquaporin protein can be distributed in a controlled fashion using PEMs, even on the inner surface of a hollow fiber membrane. In this way, various proteopolymersome multilayers (PPMs) are fabricated using PP+ as the positively charged species in combination with the polyanions poly(styrene 4-sulfonate) (PSS) and poly(acrylic acid) (PAA). It is shown by reflectometry through alternately adsorbing the polyanions and PP+ that, for both PAA and PSS, a good layer growth is possible. However, when the multilayers are imaged by SEM, the PAA-based PPMs show dewetting, whereas vesicular structures can only be clearly observed in and on the PSS-based PPMs. In addition, membrane permeability decreases upon coating the PPMs to 2.6 L∙m-2∙h-1∙bar-1 for PAA/PP+ and 7.7 L∙m-2∙h-1∙bar-1 for PSS/PP+. Salt retentions show that PAA/PP+ layers are defective (salt retentions <10% and high molecular weight cut-off (MWCO)), in line with the observed dewetting behavior, while PPMs based on PSS show 80% MgSO4 retention in combination with a low MWCO. The PSS/PP+ membranes show a Donnan-exclusion behavior with moderate MgCl2 retention (50%-55%) and high Na2SO4 retention (85%-90%) indicating a high amount of negative charge present within the PPMs. The corresponding PEMs, on the other hand, are predominately positively charged with MgCl2 retention of 97%-98% and Na2SO4 retention of 57%-80%. This means that the charge inside the multilayer and, thus, its separation behavior can be changed when PP+ is used instead of a polycation. When comparing the PPM membranes to the literature, similar performances are observed with other biomimetic membranes that are not based on interfacial polymerization, but these are the only ones prepared using a desired hollow fiber geometry. Combining PEMs and biomimetic approaches can, thus, lead to relevant membranes, especially adding to the versatility of both systems.

Dataset Information

In Vitro Bioeffects of Polyelectrolyte Multilayer Microcapsules Post-Loaded with Water-Soluble Cationic Photosensitizer.

Publications

In Vitro Bioeffects of Polyelectrolyte Multilayer Microcapsules Post-Loaded with Water-Soluble Cationic Photosensitizer.

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