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PubMedDate not supplied

Redox reaction of poly(ethylene oxide)-modified hemoglobin in poly(ethylene oxide) oligomers at 120 degrees C.

Human hemoglobin, modified with poly(ethylene oxide) with average molecular weight of 3500 (PEO-Hb) was dissolved in PEO200 (molecular weight of 200) containing 0.5 M KCl. A quasi-reversible redox reaction of the PEO-Hb was found in PEO oligomers by alternatingly changing the potential polarity (+/- 1.2 V vs Ag). The PEO-Hb showed redox reactions in PEO200 even at 120 degrees C. PEO modification was concluded to give the thermal stability in some extent. In phosphate buffer at 70 degrees C, the electrochemical redox reaction of native Hb was not observed spectroscopically, but that of PEO-Hb was detected. The most effective factor was, however, concluded to be the use of PEO oligomers as a solvent. The molecular motion of PEO oligomers should be milder than that of water at higher temperature. This lower molecular motion was suggested to keep the redox activity of PEO-Hb in the PEO oligomer at 120 degrees C. However, the PEO-Hb in PEO200 was stable in the oxidized form at 30 degrees C; it was reduced without giving potential at 120 degrees C. Cyclic voltammetry revealed that this autoreduction was attributed to the shift of redox potential with elevating temperature.

Electrochemistry↗
PubMedDate not supplied

Formyl-ended heterobifunctional poly(ethylene oxide): synthesis of poly(ethylene oxide) with a formyl group at one end and a hydroxyl group at the other end.

Well-defined poly(ethylene oxide) (PEO) with a formyl group at one end and a hydroxyl group at the other terminus was synthesized by the anionic ring opening polymerization of ethylene oxide (EO) with a new organometallic initiator possessing an acetal moiety, potassium 3,3-diethoxypropyl alkoxide. Hydrolysis of the acetal moiety produced a formyl group-terminated heterobifunctional PEO with a hydroxyl group at the other end.

Chromatography, Gel↗
PubMedDate not supplied

Primary amino-terminal heterobifunctional poly(ethylene oxide). Facile synthesis of poly(ethylene oxide) with a primary amino group at one end and a hydroxyl group at the other end.

Well-defined poly(ethylene oxide) (PEO) with a cyano group at one end and a hydroxyl group at the other terminus was synthesized by the anionic ring opening polymerization of ethylene oxide (EO) initiated with (cyanomethyl)potassium (CMP) which was prepared by the metalation reaction of acetonitrile with potassium naphthalene in THF. Primary amino-terminal heterotelechelic PEO was obtained by the reduction of the cyano group at the end of the polymer chain by lithium aluminum hydride.

Acetonitriles↗
PubMedDate not supplied

Polyelectrolyte complex micelles composed of c-raf antisense oligodeoxynucleotide-poly(ethylene glycol) conjugate and poly(ethylenimine): effect of systemic administration on tumor growth.

An antisense oligodeoxynucleotide (ODN) delivery system based on polyelectrolyte complex (PEC) micelles composed of an ODN-poly(ethylene glycol) (PEG) conjugate and polyethylenimine (PEI) was demonstrated. The PEC micelles having a core/shell structure were spontaneously formed in an aqueous solution by ionic interactions between ODN part in the conjugate and PEI. The ODN/PEI polyelectrolyte complex formed an inner core while PEG chains surrounded it as a shell. The morphology of the micelles was visualized as a separate sphere by atomic force microscopy (AFM). When the micelles containing a c-raf antisense ODN were intravenously administered into tumor-bearing nude mice, significant antitumor activities against human lung cancer were observed. The intravenously injected micelles also showed significantly higher accumulation level in the solid tumor region compared to that of naked ODN.

Animals↗
PubMedDate not supplied

Influence of polyethylene glycol chain length on the physicochemical and biological properties of poly(ethylene imine)-graft-poly(ethylene glycol) block copolymer/SiRNA polyplexes.

Polyplexes between siRNA and poly(ethylene imine) (PEI) derivatives are promising nonviral carriers for siRNA. The polyplex stability is of critical importance for efficient siRNA delivery to the cytoplasm. Here, we investigate the effect of PEGylation at a constant ratio ( approximately 50%) on the biophysical properties of the polyplexes. Particle size, zeta potential, and stability against heparin as well as RNase digestion and reporter gene knockdown under in vitro conditions of different siRNA polyplexes were characterized. Stability and size of siRNA polyplexes were clearly influenced by PEI-PEG structure, and high degrees of substitution such as PEI(25k)-g-PEG(550)(30) resulted in large (300-400 nm), diffuse complexes (AFM) which showed condensation behavior only at high N/P ratios. All other polyplexes and the PEI control showed similar sizes (150 nm) and compact structures in AFM, with complete condensation reached at N/P ratio of 3. Stability of siRNA polyplexes against heparin displacement and RNase digestion could be modified by PEGylation. Protection against RNase digestion was highest for PEI(25k)-g-PEG(5k)(4) and PEI(25k)-g-PEG(20k)(1), while siRNA/PEI provided insufficient protection. In knockdown experiments using NIH/3T3 fibroblasts stably expressing beta-galactosidase, it was shown that PEG chain length had a significant influence on biological activity of siRNA. Polyplexes with siRNA containing PEI(25k)-g-PEG(5k)(4) and PEI(25k)-g-PEG(20k)(1) yielded similar efficiencies of ca. 70% knockdown as lipofectamine controls. Confocal microscopy demonstrated enhanced cellular uptake of siRNA into cytosol by polyplexes formation with PEI copolymers. In conclusion, both the chain length and graft density of PEG were found to strongly influence siRNA condensation and stability and hence affect the knockdown efficiency of PEI-PEG/siRNA polyplexes.

Animals↗
PubMedDate not supplied

Effect of cast solvent on the electron transfer reaction for poly(ethylene oxide)-modified myoglobin on the electrode in poly(ethylene oxide) oligomers.

Myoglobin from horse skeletal muscle was modified with poly(ethylene oxide) (PEO) with an average molecular weight of 2000 or 5000. Myoglobin was soluble after this modification in several organic solvents and PEO oligomers. The electron transfer reactions of PEO-modified myoglobin cast on the indium tin oxide (ITO) glass electrode were investigated by cyclic voltammetry. The PEO-modified myoglobin, cast on the electrode from water or a methanol solution, showed quasi-reversible redox reactions in PEO (average MW of 400). On the other hand, no redox response was seen in PEO-modified myoglobin cast on it using chloroform or benzene as a casting solvent. A clear redox response of the PEO-modified myoglobin was observed after methanol treatment of these layers cast from chloroform or a benzene solution. This suggests that the conformational change of the adsorbed PEO-modified myoglobin layer on the ITO electrode cast from chloroform or a benzene solution was not irreversible. The cast condition of PEO-modified myoglobin on the ITO glass electrode was revealed to affect the electron transfer reaction for protein considerably in PEO oligomers.

Animals↗
PubMedDate not supplied

Poly(ethylene glycol)-block-poly(L-lysine) dendrimer: novel linear polymer/dendrimer block copolymer forming a spherical water-soluble polyionic complex with DNA.

Methoxypoly(ethylene glycol)-block-poly(L-lysine) dendrimer was designed to form a water-soluble complex with plasmid DNA. The copolymer was synthesized by the liquid-phase peptide synthesis method. It was characterized by 1H NMR and matrix-assisted laser desorption ionization-time-of-flight (MALDI-TOF) mass spectrum. Agarose gel electrophoresis and DNase I protection assay proved that this linear polymer/dendrimer block copolymer assembled spontaneously with plasmid DNA, forming a water-soluble complex which increased the stability of the complexed DNA. Atomic force microscopy of the complex was evaluated at various charge ratios showing that the copolymer/DNA complex was like a globular shape.

DNA↗
PubMedDate not supplied

Poly(ethylene glycol)-modification of the phospholipid vesicles by using the spontaneous incorporation of poly(ethylene glycol)-lipid into the vesicles.

The critical micelle concentrations of 1, 2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-[monomethoxy poly(ethylene glycol) (5000)] (PEG-DPPE) and its distearoyl analogue (PEG-DSPE) were 70 and 9 microM, respectively, in buffer solutions ([Tris] = 20 mM, [NaCl] = 140 mM, pH 7.4) at 37 degrees C. When these PEG-lipid micelle dispersions were mixed with the dispersions of phospholipid vesicles comprised of a C16 membrane, of which the carbon number is 16, or a C18 membrane, the PEG-lipid micelles were dissociated into monomers and then spontaneously incorporated into the surface of the preformed vesicles. The incorporation rates and the enthalpy changes during incorporation were measured with an isothermal titration microcalorimeter. The incorporation rate of PEG-DPPE was faster than that of PEG-DSPE, because the dissociation rate of the PEG-DPPE micelles was faster than that of PEG-DSPE micelles. The incorporation equilibrium constant of PEG-DSPE was larger than that of PEG-DPPE due to its slow dissociation rate from the membrane, caused by the stronger hydrophobic interaction. The combination of PEG-DSPE and the C18 membrane was the most thermodynamically stabilized pair. Furthermore, the dispersion stability of the surface-modified vesicles prepared by this spontaneous incorporation was analyzed by using the critical molecular weight of the polymer for the aggregation of vesicles. The aggregation of the vesicles was successfully supressed with an increase in the molecular weight of the PEG in the PEG-lipid and its incorporation ratio.

Chemical Phenomena↗
PubMedDate not supplied

Amphotericin B encapsulated in micelles based on poly(ethylene oxide)-block-poly(L-amino acid) derivatives exerts reduced in vitro hemolysis but maintains potent in vivo antifungal activity.

The core-forming blocks of amphiphilic diblock copolymers based on methoxypoly(ethylene oxide)-block-poly(L-aspartate), PEO-b-p(L-Asp), were derivatized to incorporate stearate side chains. The effects of stearate esterification were assessed in terms of micelle stability and amphotericin B (AmB) encapsulation/release. The level of stearate esterification modulates the relative self-aggregation state of encapsulated AmB as evidenced by absorption spectroscopy. When AmB is physically loaded into polymeric micelles, the onset of hemolytic activity toward bovine erythrocytes is delayed relative to that of the free drug. Furthermore, the extent of esterification (0, 46, or 91%) appears to have profound influence on the time-dependent hemolytic profile of AmB toward bovine erythrocytes. Particularly in the case of highly substituted stearate ester micelles, incomplete and gradual build-up of hemolysis was observed over a period of 24 h. On the basis of the corresponding absorption spectra, we speculate that encapsulated AmB may interact strongly with stearate side chains, resulting in sustained release. In a neutropenic murine model of disseminated candidiasis, kidney colony-forming unit determination revealed dose-dependent efficacy for the polymeric micelle/AmB formulation, which was not significantly different from that of Fungizone at doses of 0.2, 0.3, and 0.6 mg/kg (p = 0.7). Thus, AmB administered via a polymeric micelle formulation retained potent in vivo activity.

Amphotericin B↗
PubMedDate not supplied

Poly(ethylene glycol)-poly(ester-carbonate) block copolymers carrying PEG-peptidyl-doxorubicin pendant side chains: synthesis and evaluation as anticancer conjugates.

Water soluble polymer anticancer conjugates can improve the pharmacokinetics of covalently bound drugs by limiting cellular uptake to the endocytic route, thus prolonging plasma circulation time and consequently facilitating tumor targeting by the enhanced permeability and retention (EPR) effect. Many of the first generation antitumor polymer conjugates used nonbiodegradable polymeric carriers which limits the molecular weight that can be safely used to <40,000 g/mol. The aim of this ambitious study was to synthesize and evaluate a novel, prototype biodegradable polymeric system based on high molecular weight, water-soluble functionalized polyesters. The main polymeric platform was prepared from bis(4-hydroxy)butyl maleate (DBM) and poly(ethylene glycol) (PEG4000) blocks to give the polymer DBM2-PEG4000 containing biodegradable carbonate bonds and having a M(w) of 100,000-190,000 g/mol; M(n) of 37,000-53,000 g/mol, and M(w)/M(n) of 3.0-3.7. Using thioether linkages, this polymer was then grafted with HS-PEG3000-Gly-Phe-Lue-Gly doxorubicin (HS-PEG3000-GFLG-Dox) pendant side chains ( approximately 30 per DBM2-PEG chain). The final construct, DBM2-PEG4000-S-PEG3000-GFLG-Dox had a total Dox content of 3-4 wt % and a free Dox content of < or = 0.7% total Dox. During incubation with isolated lysosomal enzymes, the rate of Dox release from the polymer backbone was relatively slow (<5% release over 5 h) compared to that seen for PEG5000-GFLG-Dox alone (>20% over 5 h). The in vitro cytotoxicity was assessed using B16F10 murine melanoma (MTT assay). DBM2-PEG4000-S-PEG3000-GFLG-Dox was 10-20-fold less toxic than free Dox. In vivo antitumor activity of the DBM2-PEG4000-S-PEG3000-GFLG-Dox conjugates was assessed using a subcutaneous (s.c.) B16F10 murine melanoma model, and an intraperitoneal (i.p.) L1210 leukaemia model. The increased toxicity (attributed to poor solubility) and low antitumor activity of DBM2-PEG4000-S-PEG3000-GFLG-Dox conjugates compared to PEG5000-GFLG-Dox and HPMA copolymer-Dox conjugates was attributed to the slow rate of Dox release. The DBM2-PEG4000-S-PEG3000-GFLG-Dox conjugates were considered unfavorable as candidates for further development. However, the successful scale-up synthesis of DBM2-PEG4000-S-PEG3000 constructs suggest that they are worthy of further investigation as carriers for controlled release and targeting of less hydrophobic agents.

Animals↗
PubMedDate not supplied

Poly(ethylene oxide sulfide): new poly(ethylene glycol) derivatives degradable in reductive conditions.

Poly(ethylene oxide sulfide) (PEOS), polymers consisting of an internal ethylene oxide oligomer and disulfide linkage, were synthesized and characterized. The degree of polymerization was dependent upon temperature, dimethyl sulfoxide condition, and monomer hydrophobicity. The stability of PEOS was measured by the size exclusion chromatography method after the incubation both with and without 5 mM glutathione. The disulfide bond was stable in the extracellular condition but completely degraded in 2 h in the reductive cytosolic condition. Hydrophilic PEOS polymers showed no cytotoxicity on the HepG2 cell line. On the basis of these properties, PEOS can be applied in many drug delivery fields.

Cell Line, Tumor↗
PubMed2006

Biomimetic porous scaffolds made from poly(L-lactide)-g-chondroitin sulfate blend with poly(L-lactide) for cartilage tissue engineering.

A novel biodegradable graft copolymer chondroitin sulfate-grafted poly(L-lactide) (CS-PLLA) was synthesized. The graft copolymer was blended with PLLA to form biomimetic porous scaffolds. Natural CS was introduced into the polyester matrix to promote the proliferation of cells. Three-dimensional spongelike scaffolds were fabricated by a combination of salt leaching and solvent casting methods. The morphology of the scaffolds was observed with scanning electron microscopy with an average pore size between 50 and 250 microm, and its porosity was high (>85%). Compression analysis indicated that the mechanical properties of the scaffold were adequate to support the proliferation of cells. The hydrophilicity increased with an increase in the copolymer content in the blend, as determined by measuring the contact angle. Hematoxylin and eosin, Masson, and Safranin-O staining showed that cells formed a chondro tissue gradually. Histological results revealed that abundant cartilaginous matrixes surrounded spherical chondrocytes in the center of the explants. Chondrocytes cultured in this extracellular-matrix-like scaffold maintained a round morphology phenotype, characterized by a significant quantity of extracellular matrixes of sulfated glycosaminoglycans and collagens. Additionally, phenotypic gene expression (reverse transcriptase-polymerase chain reaction) indicated that chondrocytes expressed transcripts that encoded type II collagen and aggrecan and generated sulfated glycosaminoglycans.

Aggrecans↗
PubMed2005

Soft vesicles formed by diblock codendrimers of poly(benzyl ether) and poly(methallyl dichloride).

The synthesis of a block codendrimer (g3-PBE-b-g3-PMDC), composed of a third-generation poly(benzyl ether) (PBE) monodendron and an aliphatic polyether (PMDC) monodendron is reported. In THF/diiospropyl ether (1:1) the PMDC block functions as a "hydrophilic" block, while the PBE acts as a "hydrophobic" block. The codendrimer can form interdigitated layers leading to vesicle formation. Tapping mode atomic force microscopy (AFM), dynamic light scattering (DLS), and transmission electron microscopy (TEM) were used to characterize the vesicles. The effect of molecular architecture on the formation of the interdigitated layers and vesicles was studied.

Journal Article↗
PubMed2006

Preparation and characterization of silver-poly(vinylidene fluoride) nanocomposites: formation of piezoelectric polymorph of poly(vinylidene fluoride).

In situ Ag nanoparticles are produced on reduction of Ag+ with N,N-dimethylformamide in the presence of poly(vinylidene fluoride) (PVF2). The plasmon band transition is monitored with time in the reaction mixture for three sets of experiments by UV-vis spectroscopy. The plasmon band absorbance increases sigmoidally with log(time). Analysis of the data with the Avrami equation yields an exponent n value between 1.5 and 2.0, indicating two-dimensional nucleation with linear or diffusion controlled growth. The TEM study of the polymer nanocomposites (PNC) indicates both spherical and rodlike morphology for PNC0.5 and PNC2.5 samples, whereas the PNC11 sample has spherical and agglomerated structures (the numerical number associated with PNC indicates percentage (w/w) of Ag in the nanocomposite). The WAXS and FTIR studies indicate the formation of piezoelectric beta-polymorphic PVF2 in the nanocomposites. The DSC study indicates some increase of the melting point and enthalpy of fusion of PVF2 in the nanocomposite, although with increase in Ag nanoparticle concentration the increase is smaller. The crystallization temperatures of PNCs also increased, indicating nucleating effect of Ag nanoparticles in the composite. In the TGA curves, the PNCs exhibit a three-step degradation process. The degradation temperatures of PNCs are lower than that of PVF2. The storage modulus data indicate a significant reinforcement of the mechanical property in the PNCs where also the reinforcement effect decreases with increasing nanoparticle concentration. Both the loss modulus and tan delta plots indicate two peaks; the lower temperature peak has been attributed for glass transition temperature, whereas the higher one has been attributed to a similar type relaxation process for the crystalline-amorphous interface. The increase in the glass transition is marginal for the PNCs, but the increase of later transition temperature is somewhat higher. The FTIR study shows that the dipolar interaction of the >CF2 dipole with the surface charges of Ag nanoparticle stabilizes the nanoparticle in the nanocomposite.

Journal Article↗
PubMed2004

Hydrogen-bonding-directed layer-by-layer assembly of poly(4-vinylpyridine) and poly(4-vinylphenol): effect of solvent composition on multilayer buildup.

This paper describes the buildup of hydrogen-bonding-directed poly(4-vinylpyridine)/poly(4-vinylphenol) (PVPy/PVPh) multilayer film that was fabricated by layer-by-layer (LbL) assembly of PVPy and PVPh from an ethanol solution. UV-visible spectroscopy and Fourier transform infrared (FT-IR) spectroscopy revealed a uniform deposition process. The interaction between PVPy and PVPh was identified as hydrogen bonding through FT-IR spectroscopy and temperature-dependent IR spectral changes of the hydrogen-bonded multilayer. Notably, we discussed the effect of solvent conditions on the growth of PVPy/PVPh multilayer films monitored by UV-visible spectroscopy. It was found that increasing the ratio of N,N-dimethylformamide (DMF) in the mixed ethanol/DMF solvents resulted in a marked decrease of the amount of polymers adsorbed, which was attributed to the increased polarity of the adsorption solutions. Furthermore, the solvent stability of PVPy/PVPh multilayer film in mixed ethanol/DMF solvents with different DMF ratios was also investigated. As a result, a new method for tuning the structure of hydrogen-bonding-directed multilayer film was developed.

Ethanol↗
PubMed2005

Relationship between interfacial forces measured by colloid-probe atomic force microscopy and protein resistance of poly(ethylene glycol)-grafted poly(L-lysine) adlayers on niobia surfaces.

Adsorbed layers of "comb-type" copolymers consisting of PEG chains grafted onto a poly(l-lysine) (PLL) backbone on niobium oxide substrates were studied by colloid-probe AFM in order to characterize the interfacial forces associated with coatings of varying architectures (PEG/PLL ratios and PEG chain lengths) and their relevance to protein resistance. The steric and electrostatic forces measured varied substantially with the architecture of the PLL-g-PEG copolymers. Varying the ionic strength of the buffer solutions enabled discrimination between electrostatic and steric-entropic contributions to the net interfacial force. For high PEG grafting densities the steric component was most prominent, but at low ionic strengths and high grafting densities, a repulsive electrostatic surface force was also observed; its origin was assigned to the niobia charges beneath the copolymer, as insufficient protonated amine groups in the PLL backbone were available for compensation of the oxide surface charges. For lower grafting densities and lower ionic strengths there was a substantial attractive electrostatic contribution arising from interaction of the electrical double layer arising from the protonated amine groups, with that of the silica probe surface (as under low ionic strength conditions, the electrical double layer was thicker than the PEG layer). For these PLL-g-PEG coatings the net interfacial force can thus be a markedly varying superposition of electrostatic and steric-entropic contributions, depending on various factors. The force curves correlate with protein adsorption data, demonstrating the utility of AFM colloid-probe force measurements for quantitative analysis of surface forces and how they determine interfacial interactions with proteins. Such characterization of the net interfacial forces is essential to elucidate the multiple types of interfacial forces relevant to the interactions between PLL-g-PEG coatings and proteins and to advance interpretation of protein adsorption or repellence beyond the oversimplified steric barrier model; in particular, our data demonstrate the importance of an ionic-strength-dependent minimum PEG layer thickness to screen the electrostatic interactions of charged interfaces.

Adsorption↗
PubMed2006

Simple method for the preparation of DNA-poly(o-methoxyaniline) hybrid: structure, morphology, and uncoiling of poly(o-methoxyaniline) on the DNA surface.

The DNA-poly(o-methoxyaniline) (POMA) hybrid is prepared by mixing aqueous solutions of POMA [emeraldine salt (ES), doping level [Cl]/[N] = 0.52] and sodium salt of DNA (Na-DNA) and is then freeze-dried after 4 days. Three different compositions (WDNA = 0.25, 0.5, and 0.75, WDNA is the weight fraction of DNA) of the hybrids are prepared. The SEM pictures show a gradation in morphology; for example, for WDNA = 0.75, fibrils are present but, at lower DNA concentration, a fibrillar network structure of the hybrid is observed. The circular dichroism (CD) spectra of the hybrid solutions indicate unchanged DNA conformation and WAXS patterns indicate intact crystal structure of DNA in the hybrid. The UV-vis spectra suggest no denaturation of DNA during the blending process. The UV-vis spectra of the hybrids in aqueous medium show a gradual red shift of the pi band to polaron band transition with time. The plots of these wavelengths with time are sigmoidal, indicating the autocatalytic nature of the process. With an increase in the temperature, the rate of the red shift of the above peak is faster. Arrhenius analysis of the rate (1/tau700 where tau700 is the time required to reach the absorption maximum at the wavelength 700 nm) yields straight lines for the three hybrid compositions with activation energy values of 13-15 kcal/mol. These values are almost equal to the activation energy values of conformational transition of other polymers, supporting the red shift in UV-vis spectra occurs from conformational transition. DNA offers a surface where POMA gets adsorbed and the stable conformational transition resulting in the uncoiling of the POMA chain occurs through repulsive interaction among bound radical cations of POMA (ES) on the DNA surface. The conductivity of the hybrids is on the order of 10(-6) S/cm, and the I-V characteristic curves indicate the semiconducting nature of the hybrids.

Aniline Compounds↗
PubMed2002

Poly(D,L-lactide-co-glycolide) encapsulated poly(vinyl alcohol) hydrogel as a drug delivery system.

PURPOSE: The efficiency of encapsulation of water-soluble drugs in biodegradable polymer is often low and occasionally these microcapsules are associated with high burst effect. The primary objective of this study is to develop a novel microencapsulation technique with high efficiency of encapsulation and low burst effect. METHOD: Pentamidine was used as a model drug in this study. Pentamidine/polyvinyl alcohol (PVA) hydrogel was prepared by freeze-thaw technique. Pentamidine loaded hydrogel was later microencapsulated in poly(lactide-co-glycolide) (PLGA) using solvent evaporation technique. The microcapsules were evaluated for the efficiency of encapsulation, particle size. surface morphology, thermal characteristic, and drug release. RESULT: Scanning Electron Microscope (SEM) studies revealed that the microcapsules were porous. The microcapsules were uniform in size and shape with the median size of the microcapsules ranging between 27 and 94 microm. The samples containing 10% PLGA showed nearly three times increase in drug loading (18-53%) by increasing the hydrogel content from 0-6%. The overall drug release from the microencapsulated hydrogel, containing 3% and 6% PVA, respectively. was significantly lower than the control batches. CONCLUSION: The use of a crosslinked hydrogel such as PVA can significantly increase the drug loading of highly water-soluble drugs. In addition. incorporation of the PVA hydrogel significantly reduced the burst effect and overall dissolution of pentamidine.

Drug Compounding↗