Release Of Hydrophilic Drugs Research Articles

Mechanically enhanced lipo-hydrogel with controlled release of multi-type drugs for bone regeneration

Hydrogel is an excellent candidate in the field of drug delivery and tissue regeneration. However, hydrogel used as drug carriers is facing several problems including limited optional drug and burst drug release, besides hydrogel is still confronting some challenges in mechanical property involving decreased hydrogel's strength caused by interface separation between hydrogel and other solid composition. In this research, we designed a mechanical enhanced and release-controlling liposome modified hydrogel via hydrogen bone and hydrogel network micro-cross-linking double network as artificial scaffold for promoting the angiogenesis and osteogenesis in bone regeneration. Specifically, photo-cross linkable gelatin derivative (GelMA) was combined with drug loaded liposome by bonding effects, which lead to double improvement in mechanical property, such as compression, stretching, torsion and resiliency. Furthermore, the ability to control phased release was observed in the composite hydrogel including the early release of hydrophilic drug (deferoxamine), mid-term release of bioactive macromolecule (bovine serum albumin and bone morphogenetic protein 2) and long-term release of liposoluble medicine (paclitaxel). In vitro study revealed that, this composite hydrogel significantly promoted osteogenic and angiogenesis differentiation without significant influence on cell adhesion, proliferation. Finally, the composite hydrogel demonstrated a superior capacity in accelerating new and mature lamellar bone formation in distal femoral defect of Sprague-Dawley rats. Thus, the liposome modified hydrogel could supply a promising strategy for extending the application of hydrogel in drug delivery and tissue reconstruction.

Investigation of in vitro hydrophilic and hydrophobic dual drug release from polymeric films produced by sodium alginate-MaterBi® drying emulsions

Emulsions are known to be effective carriers of hydrophobic drugs, and particularly injectable emulsions have been successfully implemented for in vivo controlled drug release. Recently, high internal phase emulsions have also been used to produce porous polymeric templates for pharmaceutical applications. However, emulsions containing dissolved biopolymers both in the oil and water phases are very scarce. In this study, we demonstrate such an emulsion, in which the oil phase contains a hydrophobic biodegradable polymer, MaterBi®, and the water phase is aqueous sodium alginate dispersion. The two phases were emulsified simply by ultrasonic processing without any surfactants. The emulsions were stable for several days and were dried into composite solid films with varying MaterBi®/alginate fractions. The films were loaded with two model drugs, a hydrophilic eosin-based cutaneous antiseptic and the hydrophobic curcumin. Drug release capacity of the films was investigated in detail, and controlled release of each model drug was achieved either by tuning the polymer fraction in the films during emulsification or by crosslinking sodium alginate fraction of the films by calcium salt solution immersion. The emulsions can be formulated to carry either a single model drug or both drugs depending on the desired application. Films demonstrate excellent cell biocompatibility against human dermal fibroblast, adult cells.

Improved design and characterization of PLGA/PLA-coated Chitosan based micro-implants for controlled release of hydrophilic drugs

Repetitive intravitreal injections of Methotrexate (MTX), a hydrophilic chemotherapeutic drug, are currently used to treat selected vitreoretinal (VR) diseases, such as intraocular lymphoma. To avoid complications associated with the rapid release of MTX from the injections, a Polylactic acid (PLA) and Chitosan (CS)-based MTX micro-implant prototype was fabricated in an earlier study, which showed a sustained therapeutic release rate of 0.2–2.0 µg/day of MTX for a period ∼1 month in vitro and in vivo. In the current study, different combinations of Poly(lactic-co-glycolic) acid (PLGA)/PLA coatings were used for lipophilic surface modification of the CS-MTX micro-implant, such as PLGA 5050, PLGA 6535 and PLGA 7525 (PLA: PGA – 50:50, 65:35, 75:25, respectively; M.W: 54,400 – 103,000) and different PLA, such as PLA 100 and PLA 250 (MW: 102,000 and 257,000, respectively). This improved the duration of total MTX release from the coated CS-MTX micro-implants to ∼3–5 months. With an increase in PLA content in PLGA and molecular weight of PLA, a) the initial burst of MTX and the mean release rate of MTX can be reduced; and b) the swelling and biodegradation of the micro-implants can be delayed. The controlled drug release mechanism is caused by a combination of diffusion process and hydrolysis of the polymer coating, which can be modulated by a) PLA content in PLGA and b) molecular weight of PLA, as inferred from Korsmeyer Peppas model, Zero order, First order and Higuchi model fits. This improved micro-implant formulation has the potential to serve as a platform for controlled release of hydrophilic drugs to treat selected VR diseases.

Development of a novel chitosan based biocompatible and self-healing hydrogel for controlled release of hydrophilic drug

Smart polymeric hydrogels of chitosan and acryloyl-phenylalanine having potential of fast intrinsic shape memory properties (self-healing), non-toxic, biocompatible with moderate mechanical strength have been developed. The hydrogel has been formed by linking its network with flexible pendant side chains of chitosan and acryloyl-phenylalanine (exhibiting optimal balance of hydrophilic and hydrophobic moieties). The non-toxic and biocompatible behavior of the synthesized chitosan based hydrogel reveals its potential use towards the biomedical field. The side chain of hydrogel consists of amine and carboxylic acid groups and these moieties allow non-covalent interactions (H-bonding) across its interface. Thus, synthesized hydrogel shows very good self-healing property. Further, it has shown remarkable swelling (at different pH viz.- 2, 7, 9), cell viability (HEK-293 cells up to 200 μg/mL), cell proliferation, and controlled drug release and thus found multi-responsive.

A comparative study of single-needle and coaxial electrospun amyloid-like protein nanofibers to investigate hydrophilic drug release behavior

In this study, nanofibers containing an amyloid-like bovine serum albumin (AL-BSA) carrier and a model drug (ampicillin) were produced by electrospinning. The release behavior of ampicillin was compared from electrospun nanofibers prepared as either coaxial or single-needle types. SEM images showed that the membranes had a uniform and smooth structure and the core/shell fibers were found to be thicker than the core fibers. Core/shell production was proved by transmission electron microscopy images. Fourier transform infrared spectroscopy indicated the existence of compatibility between ampicillin and the AL-BSA matrix. The in vitro antimicrobial properties of ampicillin were studied through the comparison of bacterial inhibition zones and ampicillin was found to be more effective against Gram-positive Staphylococcus aureus than Gram-negative Escherichia coli. Moreover, in vitro drug release tests were conducted to explore the relationship between the shell thickness and the drug release rate. A burst release was observed for all membranes owing to the small fiber diameters and thus short diffusion lengths. For core membranes, the drug release mechanism followed Fickian transport, which was close to zero-order kinetic. A typical biphasic release mechanism was observed for the core/shell nanofibers. Overall, we present the first evidence of AL-BSA as a potential core/shell drug mediator.

Preparation of Micro/Nano-fibers Membranes Encapsulated with Dual Drugs by Emulsion Electrospun and Controlled Release of Hydrophilic and Hydrophobic Drugs†

Preparation of Micro/Nano-fibers Membranes Encapsulated with Dual Drugs by Emulsion Electrospun and Controlled Release of Hydrophilic and Hydrophobic Drugs†

Phenylboronic Acid Functionalized Polycarbonate Hydrogels for Controlled Release of Polymyxin B in Pseudomonas Aeruginosa Infected Burn Wounds.

While physically crosslinked polycarbonate hydrogels are effective drug delivery platforms, their hydrophobic nature and lack of side chain functionality or affinity ligands for controlled release of hydrophilic drugs underscore the importance of their chemical compositions. This study evaluates an array of anionic hydrogel systems of phenylboronic acid functionalized triblock copolymers prepared via reversible physical interactions. Variation of key chemical functionalities while maintaining similar core structural features demonstrates the influence of the substitution position and protection of the boronic acid functionality on gel viscoelasticity and mechanical strength at physiological pH. The optimum gel systems obtained from the meta-substituted copolymers (m-PAP) are stable at physiological pH and nontoxic to mammalian dermal cells. The polymyxin B loaded m-PAP hydrogels demonstrate controlled in vitro drug release kinetics and in vitro antimicrobial activity against Pseudomonas aeruginosa over 48 h. In vivo antimicrobial efficacy of the drug loaded hydrogels further corroborates the in vitro results, demonstrating sustained antimicrobial activity against P. aeruginosa burn wound infections. The current strategy described in this study demonstrates a straightforward approach in designing physiologically relevant boronic acid hydrogel systems for controlled release of cationic antimicrobials for future clinical applications.

Nanofibers: An Effective Tool for Controlled and Sustained Drug Delivery.

Electrospun nonwoven nanofibers are emerging as a novel carrier for verity of drugs meant for treatment of infections, disorders and tissue engineering scaffolds. These systems may used widely in controlled release of drug that are beneficial for the health management. Nonwoven structures may provide great surface area, absorbable, simplistic processing and economical. For water loving small molecule drugs, their high water solubility and poor partition and compatibility issues with polymers make it long term release yet more challenging. Several strategies have been explored to control the release of hydrophilic drugs with high drug payload in electrospun fibers. Various techniques like blending, co-axial electrospinning can be used to improve drug payload. Studies have suggested that electrospinning methods are important attributes of developed nanofibers. Further, types of polymers are also important contributory factor on drug load and release. This review gives an overview of nanofibers used for controlled and sustained release for drugs. This articles enlightened that physicochemical and biological properties of nanofibers may be regulated by changing processing and formulation parameters.

Dual delivery of hydrophilic and hydrophobic drugs from chitosan/diatomaceous earth composite membranes

Oral administration of drugs presents important limitations, which are frequently not granted the importance that they really have. For instance, hepatic metabolism means an important drug loss, while some patients have their ability to swell highly compromised (i.e. unconsciousness, cancer…). Sublingual placement of an accurate Pharmaceutical Dosage Form is an attractive alternative. This work explores the use of the β-chitosan membranes, from marine industry residues, composed with marine sediments for dual sublingual drug delivery. As proof of concept, the membranes were loaded with a hydrophilic (gentamicin) and a hydrophobic (dexamethasone) drug. The physico-chemical and morphological characterization indicated the successful incorporated of diatomaceous earth within the chitosan membranes. Drug delivery studies showed the potential of all formulations for the immediate release of hydrophilic drugs, while diatomaceous earth improved the loading and release of the hydrophobic drug. These results highlight the interest of the herein developed membranes for dual drug delivery.

Micelles prepared from poly(N-isopropylacrylamide-co-tetraphenylethene acrylate)-b-poly[oligo(ethylene glycol) methacrylate] double hydrophilic block copolymer as hydrophilic drug carrier.

Self-assembled micelles obtained from a double hydrophilic block copolymer (DHBC) based on poly(N-isopropylacrylamide) (PNIPAAm) are a facile and green strategy compared to the conventional solvent exchange method. However, hydrophobic drug encapsulation in micelles from PNIPAAm-based DHBC has relatively low drug loading (DL) and encapsulation efficiency (EE). Intermolecular and intramolecular hydrogen bondings of PNIPAAm chains are formed to exclude hydrophobic drugs. Nevertheless, hydrogen bonding can be used for hydrophilic drug delivery. Therefore, we report micelles prepared from a poly(N-isopropylacrylamide-co-tetraphenylethene acrylate)-b-poly[oligo(ethylene glycol) methacrylate] [P(NIPAAm-co-TPE)-b-POEGMA] double hydrophilic block copolymer as a hydrophilic drug (thymopentin, TP5) carrier. The FTIR results confirm hydrogen bond formation between PNIPAAm chain and TP5. Micelles are obtained by simply increasing the temperature above the critical micelle temperature (CMT). The self-assembly behaviour of polymeric micelles is investigated by DLS, TEM and aggregation-induced emission (AIE) phenomenon. Cytotoxicity results indicate that the micelles are biocompatible. The in vitro prolonged drug release (from 6 min to several hours) and in vivo immunity enhancement indicate that the micelles formed by P(NIPAAm-co-TPE)-b-POEGMA DHBC are promising candidates as hydrophilic drug carriers, where hydrogen bonding is formed between PNIPAAm and drug.

Degree of Unsaturation and Backbone Orientation of Amphiphilic Macromolecules Influence Local Lipid Properties in Large Unilamellar Vesicles.

Liposomes have become increasingly common in the delivery of bioactive agents due to their ability to encapsulate hydrophobic and hydrophilic drugs with excellent biocompatibility. While commercial liposome formulations improve bioavailability of otherwise quickly eliminated or insoluble drugs, tailoring formulation properties for specific uses has become a focus of liposome research. Here, we report the design, synthesis, and characterization of two series of amphiphilic macromolecules (AMs), consisting of acylated polyol backbones conjugated to poly(ethylene glycol) (PEG) that can serve as the sole additives to stabilize and control hydrophilic molecule release rates from distearoylphosphatidylcholine (DSPC)-based liposomes. As compared to DSPC alone, all AMs enable liposome formation and stabilize their colloidal properties at low incorporation ratios, and the AM's degree of unsaturation and hydrophobe conformation have profound impacts on stability duration. The AM's chemical structures, particularly hydrophobe unsaturation, also impact the rate of hydrophilic drug release. Course-grained molecular dynamics simulations were utilized to better understand the influence of AM structure on lipid properties and potential liposomal stabilization. Results indicate that both hydrophobic domain structure and PEG density can be utilized to fine-tune liposome properties for the desired application. Collectively, AMs demonstrate the potential to simultaneously stabilize and control the release profile of hydrophilic cargo.

Hydrogen bonded niosomes for encapsulation and release of hydrophilic and hydrophobic anti-diabetic drugs: An efficient system for oral anti-diabetic formulation

A niosomal formulation for simultaneous encapsulation and release of hydrophobic and hydrophilic anti-diabetic drugs is reported. The niosomes were prepared by thin film hydration method which involved self assembly of Tween 80 and cholesterol. Confocal laser scanning microscopy (CLSM) investigations revealed that nile red (the hydrophobic molecule) preferentially accumulated in the shell while FITC-dextran (the hydrophilic molecule) loaded in the aqueous core of the niosome. Fourier transform infra-red (FTIR) spectroscopy investigation of niosomes revealed hydrogen bond formation between tween 80 and cholesterol. The encapsulation efficiencies for glipizide and metformin hydrochloride (metformin HCl) were found to be 67.64% and 58.72%, respectively. The drug release experiments performed in buffers at different pH values (mimicking the blood plasma pH, cellular endosomal and gastric environments) revealed that the drug release followed a linear profile up to 8–10 h, slowed down, and lasted for 12–14 h. Thus, this formulation offers a promising drug delivery system for combinatorial sustained release of anti-diabetic drugs.

Electrospun fibers in regenerative tissue engineering and drug delivery

Abstract Electrospinning is a versatile technique to produce micron or nano sized fibers using synthetic or bio polymers. The unique structural characteristic of the electrospun mats (ESM) which mimics extracellular matrix (ECM) found influential in regenerative tissue engineering application. ESM with different morphologies or ESM functionalizing with specific growth factors creates a favorable microenvironment for the stem cell attachment, proliferation and differentiation. Fiber size, alignment and mechanical properties affect also the cell adhesion and gene expression. Hence, the effect of ESM physical properties on stem cell differentiation for neural, bone, cartilage, ocular and heart tissue regeneration will be reviewed and summarized. Electrospun fibers having high surface area to volume ratio present several advantages for drug/biomolecule delivery. Indeed, controlling the release of drugs/biomolecules is essential for sustained delivery application. Various possibilities to control the release of hydrophilic or hydrophobic drug from the ESM and different electrospinning methods such as emulsion electrospinning and coaxial electrospinning for drug/biomolecule loading are summarized in this review.

Near-infrared light-triggered drug release from a multiple lipid carrier complex using an all-in-one strategy

The present study reports a drug delivery system comprising nanostructured lipid carrier (NLCs) within liposomes (Lip-NLCs). This multiple lipid carrier complex features laser-triggered responsive drug release. Both hydrophobic and hydrophilic drugs can be loaded into the same formulation by applying an all-in-one strategy. We hypothesized that if we loaded the hydrophobic near-infrared (NIR) dye IR780 into the liposome phospholipid bilayer, the bilayer would be disrupted by laser irradiation so that drug release would be triggered remotely at the tumor site. We used in vitro and in vivo methods to verify that laser irradiation facilitated controlled release of both hydrophobic and hydrophilic drugs. The degree of drug release triggered by NIR laser light could be adjusted by varying the laser intensity and irradiation time. Following laser treatment, hydrophilic AMD3100 was released from the aqueous liposome chamber and then bound with CXCR4 receptors on the tumor cell surface to inhibit metastasis. NLCs carrying lipophilic IR780 were also released from the aqueous chamber of liposomes and taken up into tumor cells to enhance the photothermal therapeutic effect of IR780. More importantly, Lip-NLCs loaded with IR780 and AMD3100 (IR780-AMD-Lip-NLCs) exhibited enhanced anti-tumor and anti-metastasis effects. These results suggest that Lip-NLCs are a safe and simply prepared all-in-one platform for delivery of drugs with different solubilities. This system facilitates easily controlled release of cargoes to achieve multi-functional combined therapy.

Stereocomplex poly(lactic acid) nanocoated chitosan microparticles for the sustained release of hydrophilic drugs

In this work, novel chitosan based microparticles were developed by the layer-by-layer deposition of poly(lactic acid) stereocomplex films on their surface in the view of controlling the release of encapsulated hydrophilic drugs. As first step, the quartz crystal microbalance technique was used to monitor the step-by-step deposition of the stereocomplex layers onto chitosan by evaluating the deposited mass for each layer. Chitosan microparticles, with a size ranging between 40 and 90μm, were then produced by an aerodynamically-assisted jetting technique and covered by a poly(lactic acid) stereocomplex shell. Infrared spectroscopy, wide X-ray diffraction, field emission scanning electron microscopy and contact angle measurements were used to verify the effective poly(lactic acid) adsorption onto chitosan microparticles and the stereocomplex formation. Finally, the release of a hydrophilic local anesthetic, procaine hydrochloride, from uncoated and stereocomplex-nanocoated microparticles was preliminary evaluated over a period of 15days.

Engineering hot-melt extruded solid dispersion for controlled release of hydrophilic drugs

It is often challenging to precisely manipulate the release behavior of hydrophilic drugs that is believed to be crucial for a satisfactory therapeutic outcome. The aim of this work was to regulate the dissolution of hydrophilic drug from hot-melt extruded solid dispersion via rational screening of the pore-forming agents. Venlafaxine hydrochloride and Compritol® 888 ATO was selected as the model drug and carrier excipient, respectively. Hydrophilic polyethylene glycol (PEG 6000) and polyvinylpyrolidone (PVP K30) were chosen as the transient pore-forming agents. The X-ray diffraction and thermal analysis showed that both drug and carrier existed in the crystalline form. Both types of polymers could generate pores upon dissolution test and the drug release rate was proportionally correlated to the pore-forming agent content. The mathematical modelling showed that the Ritger-Peppas model gave the best fit to the release curves, which demonstrates a diffusion-dominant release mechanism. The scanning electron microscopy and mercury intrusion porosimetry analysis proved that PVP K30 could generate large pores with low porosity, but PEG 6000 produced smaller pores with relatively high porosity. The in vivo pharmacokinetics study in rat revealed that solid dispersions containing either PEG 6000 or PVP K30 (both at 2.5%, w/w) exhibited an elevated bioavailability compared to the commercial product, Effexor® XR. The current work implied that rational screening of transient pore-forming polymer in solid dispersion could be a robust approach for controlling hydrophilic drug release.

Near-infrared light-responsive liposomal contrast agent for photoacoustic imaging and drug release applications.

Photoacoustic imaging has become an emerging tool for theranostic applications. Not only does it help in <italic<in vivo</italic<, noninvasive imaging of biological structures at depths but it can also be used for drug release and therapeutic applications. We explore near-infrared light-sensitive liposomes coated with gold nanostars (AuNSs) for both imaging and drug release applications using a photoacoustic imaging system. Being amphiphilic, the liposomes lipid bilayer and the aqueous core enable encapsulation of both hydrophobic and hydrophilic drugs. The AuNSs on the surface of the liposomes act as photon absorbers due to their intrinsic surface plasmon resonance. Upon excitation by laser light at specific wavelength, AuNSs facilitate rapid release of the contents encapsulated in the liposomes due to local heating and pressure wave formation (photoacoustic wave). Herein, we describe the design and optimization of the AuNSs-coated liposomes and demonstrate the release of both hydrophobic and hydrophilic model drugs (paclitaxel and calcein, respectively) through laser excitation at near-infrared wavelength. The use of AuNSs-coated liposomes as contrast agents for photoacoustic imaging is also explored with tissue phantom experiments. In comparison to blood, the AuNSs-coated liposomes have better contrast (approximately two times) at 2-cm imaging depth.

Investigations on porous PLA composite scaffolds with amphiphilic block PLA‐b‐PEG to enhance the carrying property for hydrophilic drugs of excess dose

ABSTRACTTo address concern of the dispersion property of hydrophilic drugs of excess dose loaded in a hydrophobic poly(lactic acid) (PLA) matrix, this work developed a PLA and PLA‐b‐polyethylene glycol (PEG) composite scaffold ( ) and studied its carrier properties for aspirin as a model hydrophilic drug. The porous functional scaffolds were prepared from PLA and PLA‐b‐PEG solutions with the dose of 5, 10, and 15 wt % aspirin preloaded. The products and control samples of pure PLA with the same loading amount for comparison were characterized by scanning electron microscopy and X‐ray diffraction to examine the miscibility and porous structure. Rapid degradations in a strongly basic solution were performed to determine the actual loading amount and the encapsulation ratio. The in vitro release in phosphate buffer saline (PBS) at 37.5 °C indicated that the addition of amphiphilic block polymer may efficiently enhance the dispersion property and stabilize the release of hydrophilic drugs, especially with a high loading dose. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017, 134, 44489.

Design of smart GE11-PLGA/PEG-PLGA blend nanoparticulate platforms for parenteral administration of hydrophilic macromolecular drugs: synthesis, preparation and in vitro/ex vivo characterization

Active drug targeting and controlled release of hydrophilic macromolecular drugs represent crucial points in designing efficient polymeric drug delivery nanoplatforms. In the present work EGFR-targeted polylactide-co-glycolide (PLGA) nanoparticles were made by a blend of two different PLGA-based polymers. The first, GE11-PLGA, in which PLGA was functionalized with GE11, a small peptide and EGFR allosteric ligand, able to give nanoparticles selective targeting features. The second polymer was a PEGylated PLGA (PEG-PLGA) aimed at improving nanoparticles hydrophilicity and stealth features. GE11 and GE11-PLGA were custom synthetized through a simple and inexpensive method. The nanoprecipitation technique was exploited for the preparation of polymeric nanoparticles composed by a 1:1weight ratio between GE11-PLGA and PEG-PLGA, obtaining smart nanoplatforms with proper size for parenteral administration (143.9±5.0nm). In vitro cellular uptake in EGFR-overexpressing cell line (A549) demonstrated an active internalization of GE11-functionalized nanoparticles. GE11-PLGA/PEG-PLGA blend nanoparticles were loaded with Myoglobin, a model hydrophilic macromolecule, reaching a good loading (2.42% respect to the theoretical 4.00% w/w) and a prolonged release over 60days. GE11-PLGA/PEG-PLGA blend nanoparticles showed good in vitro stability for 30days in physiological saline solution at 4°C and for 24h in pH 7.4 or pH 5.0 buffer at 37°C respectively, giving indications about potential storage and administration conditions. Furthermore ex vivo stability study in human plasma using fluorescence Single Particle Tracking (fSPT) assessed good GE11-PLGA/PEG-PLGA nanoparticles dimensional stability after 1 and 4h. Thanks to the versatility in polymeric composition and relative tunable nanoparticles features in terms of drug incorporation and release, GE11-PLGA/PEG-PLGA blend NPs can be considered highly promising as smart nanoparticulate platforms for the treatment of diseases characterized by EGFR overexpression by parenteral administration .

Amine‐modified poly(vinyl alcohol) as a novel surfactant to modulate size and surface charge of poly(lactide‐co‐glycolide) nanoparticles

AbstractPoly(lactide‐co‐glycolide) (PLGA) nanoparticles (NPs) represent a promising tool for effective delivery of biomacromolecules, thanks to their biodegradability and biocompatibility properties. PLGA NPs are often synthesized by the emulsion‐solvent evaporation method and poly(vinyl alcohol) (PVA) represents one of the most commonly used surfactants. Although PVA‐mediated synthesis of PLGA NPs is effective in tailoring NP size and stability, the resulting negative surface charge can prevent both endosomal escape and biomacromolecule release in cell cytosol. To overcome this limit, a novel amino‐modified PVA (amino‐PVA) surfactant with a cationic charge was synthesized and its potential for the formulation of PLGA NPs was investigated. In either single (oil‐in‐water) or double (water‐in‐oil‐in‐water) emulsion synthesis, different mixtures of PVA and amino‐PVA were studied, by monitoring their effects on NP size and surface charge. Optimized properties were obtained with a combination of 0.975% (w/v) of PVA with 0.025% (w/v) of amino‐PVA. This formulation was further investigated for degradation properties and cytocompatibility. High stability and low cytotoxicity make the system promising for the encapsulation and release of hydrophilic drugs and biomacromolecules. © 2016 Society of Chemical Industry