Biodegradable Alginate Polyelectrolyte Capsules As Plausible Biocompatible Delivery Carriers

Abstract

Polyelectrolyte capsules made of different biodegradable and nonbiodegradable polymers can be designed as systems for effective encapsulation and delivery of compounds. The objective of this work was to synthesize biocompatible and biodegradable capsules (<1 μm) by the layer-by-layer (LbL) approach using alginate (ALGI) and poly-L-arginine (PARG) polyelectrolytes with a pH-sensitive outer layer of EUDRAGIT L 100 (EuL) polymer. Those capsules were loaded with curcumin as a model therapeutic drug, which possesses antioxidant, anti-inflammatory, and anticancer activity. Encapsulation of drugs inside capsules protects its therapeutic activity and increases its bioavailability. We report the capsule stability, loading efficiency, drug release, as well as capsule degradation studies as a function of pH. Furthermore, in vitro biocompatibility studies of capsules including cell viability and uptake studies were performed using HeLa cells. The here synthesized capsules exhibited good reproducibility, spherical shape, and high monodispersibility. The capsules showed good loading efficiency and drug release profile dependent upon pH environment. The in vitro studies indicate that the capsules exhibited acceptable biocompatibility and are highly internalized by cells. Our study thus suggests that alginate LbL capsules could be used as an efficient drug carrier with effective encapsulation and successful in vitro release of cargo in the cell.

Development of Silica-Based Biodegradable Submicrometric Carriers and Investigating Their Characteristics as in Vitro Delivery Vehicles

“…In order to perform a biological characterization of the synthesized capsule carriers, their cellular uptake [ 46 , 47 ], impact on cell viability and proliferation [ 11 , 48 ], their degradation [ 49 , 50 ], and their use for delivering encapsulated bioactive molecular cargo [ 15 , 51 ] were studied.…”

Quantitative Assessment of Endosomal Escape of Various Endocytosed Polymer‐Encapsulated Molecular Cargos upon Photothermal Heating

“…log P is the estimated logarithm of the partition coefficient, reflecting a chemical's partition between n-octanol and water, which can be used as an indicator to describe the hydrophobicity. [42] The following molecular cargos are enlisted and previous reports about their encapsulation are referenced: HPTS: 8-hydroxypyrene-1,3,6-trisulfonic acid trisodium salt, DHPDS: 6,8-dihydroxy-1,3-pytenedisulfonic acid disodium salt, ANTS: 8-aminonaphthalene-1,3,6-trisulfonic acid, CR110: carboxyrhodamine 110 hydrochloride, 2-NBDG: 2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose, EB: ethidium bromide, PI: propidium iodide, [4] EthD-1: ethidium homodimer-1, DAPI: 4′,6-diamidine-2′-phenylindole dihydrochloride, [4] DOX: doxorubicin, [15] DEX: dextran, [3,4,11,12,21,32] curcumin, [14] PEI: branched polyethylenimine, [16] FITC: fluorescein isothiocynate, PAH: poly(allylamine hydrochloride), [12,43] WGA: wheat germ agglutinin, [4] GFP: green fluorescent protein, [21] BSA: bovine serum albumin, [15] nucleic acid [11,15,16] such as siRNA, peptides [4] such as phalloidin-Atto565 and FAM-GRGD, nanoparticles [28,44] such as quantum dots, Au clusters, and FluoSphere. a Relative weight-average molecular weight (M w ) measured by light scattering according to Sigma Aldrich.…”

“…The encapsulation of hydrophobic molecular cargos was done by following previously reported strategies. [14,56] We incubated capsules with curcumin or coumarin 343 in ethanol for 1.5 h, and subsequently washed the capsules with water. Afterward, SR-B as a reference was encapsulated by postloading and heat-shrinking.…”

“…Capsules prepared from nondegradable polyelectrolytes, e.g., poly(allylamine) (PAH) and poly(styrenesulfonate) (PSS), protect the molecular cargo from enzymatic degradation and subsequent exocytosis. [13] Using biodegradable polyelectrolytes, part of the molecular cargo is released from the capsules [13,14] and some fraction is translocated from the lysosomes to the cytosol. [15,16] For translocation from lysosomes to the cytosol the lysosomal membrane has to be passed, which in principle is possible by chemically induced transient poration (e.g., via the use of strongly cationic polymers [17] or biodegradable silica shell [15] ).…”

Conformation of a single polyelectrolyte in poor solvents

“…Polyelectrolytes (PEs) are polymers with charged repeating units, which have attracted widespread attention in both academic and industrial research. [1][2][3][4] Applications for PEs are ubiquitous, such as surfactants in a variety of personal care/health products, 5 surface-modifiers in water treatment and oil recovery, 6,7 additives in foods, 8,9 superabsorbers in agriculture and sanitation, 10 biomedical materials in implant coating and drug delivery, 11,12 and electrolytes in lithium batteries. 13,14 In addition, many biomacromolecules, like proteins, DNA, and RNA, are essentially PEs.…”