Preparation of poly(vinyl alcohol) and hydroxypropyl‐β‐cyclodextrin inclusion complex through polymer processing

In this study, inclusion complexes (ICs) between host hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) and guest poly(vinyl alcohol) (PVA) were prepared through polymer processing with water as plasticizer and solvent. The structure of PVA/HP‐β‐CD ICs was confirmed by FTIR, ¹H‐NMR and 2D‐NOESY NMR. The yields of PVA/HP‐β‐CD ICs were 62.5%, 51.4%, and 46.8% in twin‐screw, rotor and single‐screw processing, respectively. The crystallinity, thermal properties and mechanical properties of the PVA/HP‐β‐CD ICs were characterized by X‐ray diffraction, differential scanning calorimetry, thermal gravimetric analysis and tensile tests, respectively. The results indicated that HP‐β‐CD could establish strong interfacial interaction with PVA through hydrogen bonding and form ICs with PVA. As a result, crystallinity and melting temperature decomposition temperature of PVA were decreased. Compared with pure PVA, PVA/HP‐β‐CD ICs exhibited remarkable improvement in thermal stability. Moreover, the tensile strength, elongation at break and torque of ICs with different content of HP‐β‐CD were discussed. POLYM. ENG. SCI., 55:1988–1993, 2015. © 2014 Society of Plastics Engineers     

Preparation and characterization of chitosan based hydrogels containing cyclodextrin inclusion compounds or nanoemulsions of thyme oil

Hydrogels derived from natural polysaccharides are ideal scaffolds for use in biomedical applications. pH‐sensitive polyvinyl alcohol and chitosan hydrogels containing inclusion compounds of thyme oil (TM) with host methyl‐β‐cyclodextrin (MβCD) and hydroxypropyl‐β‐cyclodextrin (HβCD) and TM nanoemulsion (TM‐nano) were prepared via controlled, biocompatible and low cost freeze–thaw method. The structure of the hydrogels was characterized by Fourier transform IR spectroscopy and optical and scanning electron microscopy. The physicochemical properties of the hydrogels such as gel fraction, swelling ratio and tensile properties were measured. The water vapor transmission rate of the hydrogels indicated that they can maintain a moist environment over the wound bed. Encapsulation and release of antibacterial TM from the hydrogels were determined by UV spectroscopy. In all cases, hydrogels with lower amounts of TM evidenced slower and more controlled release. Different kinetic models were applied for evaluating the drug release mechanism. The antibacterial activity of the samples was studied by counting the number of both Gram‐negative and Gram‐positive bacteria surviving in a broth medium and the results proved the antibacterial activity of all prepared hydrogels. The results of an MTT (3‐(4,5‐dimethylthiazol‐2yl)‐2,5‐diphenyltetrazolium bromide) assay indicated more cell viability of TM‐nano hydrogels in comparison with those of TM‐βCD inclusion compounds. Cell attachment observations also showed great biocompatibility of TM‐nano hydrogels. The prepared hydrogels, especially those containing TM‐nano, might be used as potential wound dressings to improve the wound healing process. © 2019 Society of Chemical Industry     

Release behavior from hydrogen‐bonded polymer gels prepared by pressurization

Our previous research showed that a simple ultra‐high‐pressure process made poly(vinyl alcohol) (PVA) solution into a macrogel and nanoparticles. To investigate the release properties of PVA hydrogels prepared by the ultra‐high‐pressure treatment, we prepared hydrogels containing model drugs by pressurizing a PVA solution with Alfa‐G Hesperidin or Oil Blue N as a water‐soluble or an oil‐soluble model drug, respectively. In the case of the oil‐soluble drug, an oil‐in‐water emulsion, Oil Blue N containing dodecane in a PVA solution, was used by homogenization before pressurization. The average diameter and the diameter distribution of oil droplets before and after the ultra‐high‐pressure treatment were almost the same. However, the PVA hydrogel prepared at 10,000 atm for 10 min exhibited the slowest release rate of model drugs. Thus, we found that the release rates of the model drugs from the PVA hydrogels were controlled by the degree of crosslinking in the resulting gels, which was determined from the operation parameters of the ultra‐high‐pressure treatment, such as the pressure, time, and concentration of the PVA solution. Therefore, an ultra‐high‐pressure process is promising for drug‐carrier development because of the nonharmful simple preparation process. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2011     

Poly(HEMA)/cyclodextrin‐based hydrogels for subconjunctival delivery of cyclosporin A

To enhance the solubility and ocular permeability of immunosuppressive agent, cyclosporine A (CsA), three types of delivery systems were prepared using (2‐hydroxypropyl)‐β‐cyclodextrin (HPβCD), and 2‐hydroxyethyl methacrylate (HEMA). Those systems are (i) hydrogels of HPβCD with crosslinking agent ethylene glycol diglycidylether, (ii) poly(HEMA) hydrogels, and (iii) different amounts of HPβCD‐containing poly(HEMA) hydrogels indicated as poly(HEMA‐co‐HPβCD). In the presence of HEMA, hydrogels have desired mechanical integrity with lower equilibrium content than that of hydrogels without HEMA. CsA was loaded into the HPβCD‐based hydrogels by embedding from its aqueous suspensions in higher amounts than that of the poly(HEMA) hydrogels that were loaded by CsA–HPβCD complex solution. Although the poly(HEMA) hydrogels are releasing total CsA in 3 days, long‐term release was realized from HPβCD‐based hydrogels. For subconjunctival administration, regarding to the amounts of loaded CsA, release profiles, and mechanical integrity, the most suitable system is poly(HEMA‐co‐HPβCD) hydrogels in high HPβCD content. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40397.     

Preparation,characterization, and salicylic acid release behavior of chitosan/poly(vinyl alcohol) blend microspheres

Blend microspheres of chitosan (CS) with poly(vinyl alcohol) (PVA) were prepared as candidates for oral delivery system. CS/PVA microspheres containing salicylic acid (SA), as a model drug, were obtained using the coacervation‐phase separation method, induced by addition of a nonsolvent (sodium hydroxide solution) and then crosslinked with glutaraldehyde (GA) as a crosslinking agent. The microspheres were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry (DSC), and scanning electron microscopy. Percentage entrapment efficiency, particle size, and equilibrium swelling degree of the microsphere formulations were determined. The results indicated that these parameters were changed by preparation conditions of the microspheres. Effects of variables such as CS/PVA ratio, pH, crosslinker concentration, and drug/polymer (d/p) ratio on the release of SA were studied at three different pH values (1.2, 6.8, and 7.4) at 37°C. It was observed that SA release from the microspheres increased with decreasing CS/PVA ratio and d/p ratio whereas it decreased with the increase in the extent of crosslinking. It may also be noted that drug release was much higher at pH 1.2 than that of at pH 6.8 and 7.4. The highest SA release percentage was obtained as 100% for the microspheres prepared with PVA/CS ratio of 1/2, d/p ratio of 1/2, exposure time to GA of 5 min, and concentration of GA 1.5% at the end of 6 h. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2009     

Retention of Eucalyptol,a Natural Volatile Insecticide,in Delivery Systems Based on Hydroxypropyl‐β‐Cyclodextrin and Liposomes

Eucalyptol (Euc) is a natural monoterpene with insecticide effects. Being highly volatile and sensitive to ambient conditions, its encapsulation would enlarge its application. Euc‐loaded conventional liposomes (CL), cyclodextrin/drug inclusion complex, and drug‐in‐cyclodextrin‐in‐liposomes (DCL) are prepared to protect Euc from degradation, reduce its evaporation, and provide its controlled release. The liposomal suspension is freeze‐dried using hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) as cryoprotectant. The liposomes are characterized before and after freeze‐drying. The effect of Euc on the fluidity of liposomal membrane is also examined. A release study of Euc from delivery systems, in powder and reconstituted forms, is performed by multiple head extraction at 60 °C after 6 months of storage at 4 °C. CL and DCL suspensions are homogeneous, show nanometric vesicles size, spherical shape, and negative surface charge before and after freeze‐drying. Moreover, HP‐β‐CD does not affect the fluidity of liposomes. CL formulations present a weak encapsulation for Euc. The loading capacity of eucalyptol in DCL is 38 times higher than that in CL formulation. In addition, freeze‐dried DCL and HP‐β‐CD/Euc inclusion complex show a higher retention of eucalyptol than CL delivery system. Both carrier systems HP‐β‐CD/Euc and Euc‐loaded DCL decrease Euc evaporation and improve its retention. Practical Applications: Eucalyptol is a natural insecticide. It is highly volatile and poorly soluble in water. To enlarge its application, its encapsulation in three delivery systems (conventional liposomes, cyclodextrin/drug inclusion complex, combined system composed of cyclodextrin inclusion complex and liposome) is studied. In this paper it is proved that cyclodextrin/eucalyptol inclusion complex and eucalyptol‐in‐cyclodextrin‐in‐liposome are effective delivery systems for encalyptol encapsulation, retention, and release.     

β‐cyclodextrin‐conjugated hyaluronan hydrogel as a potential drug sustained delivery carrier for wound healing

In order to develop a potential drug sustained delivery carrier suitable for wound healing, a series of β‐cyclodextrin conjugated hyaluronan hydrogels (β‐CD‐HA) with adjustable crosslink densities were synthesized and characterized, meanwhile the delivery kinetics and mechanism of diclofenac as a model anti‐inflammatory drug from these hydrogels were investigated. By controlling the feeding molar ratio of β‐CD/HA, a β‐CD substitution degree of 4.65% was obtained by ¹H‐NMR analysis. The incorporation of β‐CD modification had little effect on the internal porous structure, water swelling ratio, and rheological property of HA hydrogel, which however were influenced by the crosslink density. Although the crosslink density had an influence on the drug loading and release profile by altering the water swelling property, the interaction between β‐CD and drug was the primary factor for the high loading capacity and long‐term sustained delivery of diclofenac. The semiempirical equation fit showed that the release of diclofenac from HA‐based hydrogels followed a pseudo‐Fickian diffusion mechanism. By the aid of β‐CD and controlled crosslink density, a β‐CD‐HA hydrogel with a diclofenac sustained delivery period of over 28 days and desirable physicochemical properties was achieved, which will be a promising drug sustained delivery carrier for wound healing. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 43072.     

Fabrication of citric acid crosslinked β‐cyclodextrin/hydroxyethylcellulose hydrogel films for controlled delivery of poorly soluble drugs

β‐cyclodextrin grafted hydroxyethylcellulose (βCD‐g‐HEC) hydrogel films were prepared for the controlled release of poorly soluble model drug (ketoconazole) using citric acid as crosslinking agent. The active βCD and carboxyl content of the hydrogel films were determined by phenolphthalein assay and acid–base titration. The films were characterized by solid state ¹³C NMR, ATR–FTIR, thermogravimetric analysis, and differential scanning calorimetric, and analyzed for tensile strength, swelling ratio, drug loading, release, hemocompatibility, in vitro cytotoxicity, and implantation test. An increase in the concentration of βCD in feed increased the active βCD content of the hydrogel films but reduced their extent of interpolymer crosslinking. The βCD‐g‐HEC hydrogel films with high active βCD content showed maximum drug loading whereas those with high crosslinking density were capable of controlling the drug release for long duration. Hemolysis assay and in vitro cytotoxicity study revealed the biocompatible nature of the hydrogel films whereas implantation test indicated their minimal inflammatory effect. From the overall results, βCD‐g‐HEC hydrogel films were found to be better alternative to the previously reported βCD‐HPMC and βCD‐CMC hydrogel films for enhanced loading and long‐term release, respectively, of the poorly soluble drugs. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46452.     

Nonoxynol‐9‐α‐cyclodextrin inclusion compound and its application for the controlled release of nonoxynol‐9 spermicide

Nonoxynol‐9 (N‐9) is the most active ingredient in commercially available spermicidal products in the United States. There are many applications of cyclodextrin inclusion complexes (CD‐ICs), but there are no reported studies investigating the formation of and controlled release from a N‐9 spermicide‐CD‐IC. We have successfully formed the inclusion compound between N‐9 and α‐CD using a solution‐heating technique. The N‐9‐α‐CD‐IC was characterized by Fourier Transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, differential scanning calorimetry, thermogravimetric analysis, and wide angle X‐ray diffraction observations. Silicone elastomer (SILASTIC MDX4‐4210) film embedded with crystalline N‐9‐α‐CD‐IC was prepared and evaluated for its efficacy in the controlled release of N‐9 spermicide against bovine sperm. Silicone elastomer with N‐9‐α‐CD‐IC was as successful in reducing the motility and viability of bovine spermtazoa as silicone elastomer swollen with an equivalent amount of neat N‐9. The permeability of the flexible silicone elastomer apparently enables the N‐9 spermicide to diffuse from its embedded inclusion complex crystals to contact, immobilize, and kill bovine sperm cells. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2007     

Synthesis and properties of hydrogels of poly(acrylic‐co‐acroloyl β‐cyclodextrin)

Novel acrylic monomers (β‐CD‐A and β‐CD‐6‐EA) containing β‐cyclodextrin (β‐CD) with different extent of substitution were prepared by using dicyclohexylcarbodiimide (DCC) as a condensation agent at room temperature. Two kinds of functional hydrogels were also synthesized by copolymerization of β‐CD‐A and β‐CD‐6‐EA with acrylic acid (AAc) using a redox initiator system in aqueous solution. The nuclear magnetic resonance (¹H NMR), infrared spectroscopy (IR), thermogravimetric analysis (TGA) were employed to character the molecular structures of β‐CD modified monomers and their copolymers. The swelling experiments indicate that the hydrogels with different equilibrium swelling ratio (ESR) possess obvious pH‐sensitivity and distinct dynamic swelling behavior. Using an anti‐cancer drug, chlorambucil (CHL), able to form complexes with β‐CD in water, as a model compound, the controlled drug release behaviors of these hydrogels were investigated. The release behavior of CHL from two kinds of hydrogels synthesized reveals that the release rate of CHL can be effectively controlled by pH values, cross‐linking density, and β‐CD content. In addition, it is found that the β‐CD with the proper frame and concentration can increase release efficiency of CHL from the hydrogels. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2009     

Drug‐release behavior of chitosan‐g‐poly(vinyl alcohol) copolymer matrix

Chitosan‐g‐poly(vinyl alcohol) (PVA) copolymers with different grafting percent were prepared by grafting water‐soluble PVA onto chitosan. The drug‐release behavior was studied using the chitosan‐g‐PVA copolymer matrix containing prednisolone in a drug‐delivery system under various conditions. The relationship between the amount of the released drug and the square root of time was linear. From this result, the drug‐release behavior through the chitosan‐g‐PVA copolymer matrix is shown to be consistent with Higuchi's diffusion model. The drug‐release apparent constant (K_H) was slightly decreased at pH 1.2, but increased at pH 7.4 and 10 according to the increasing PVA grafting percent. Also, K_H was decreased by heat treatment and crosslinking. The drug release behavior of the chitosan‐g‐PVA copolymer matrix was able to be controlled by the PVA grafting percent, heat treatment, or crosslinking and was also less affected by the pH values than was the chitosan matrix. © 1999 John Wiley & Sons, Inc. J Appl Polym Sci 74: 458–464, 1999     

PLA Microspheres-Embedded PVA Hydrogels Prepared by Gamma-Irradiation and Freeze-Thaw Methods as Drug Release Carriers

A drug delivery system based on poly (vinyl alcohol) (PVA) hydrogels containing ibuprofen-loaded poly (lactic acid) (PLA) microspheres was developed to improve the release kinetics of this model drug. Gamma-irradiation and freeze-thawing were applied to prepare poly (vinyl alcohol) hydrogels. Properties and morphology of these composite hydrogels were investigated using FTIR, DSC, and SEM. In vitro release indicated that entrapment of the microspheres into the PVA hydrogels causes a reduction in both the release rate and the initial burst effect. PLA microspheres entrapped into the PVA hydrogels showed more suitable controlled release kinetics for drug delivery.     

Benzophenone incorporated polyvinyl alcohol hydrogels as photo‐induced antimicrobial materials

Photoactive antimicrobial hydrogels were produced by incorporating benzophenone (BP) into glutaraldehyde (GA) crosslinked polyvinyl alcohol (PVA). Structural and functional properties of the BP incorporated PVA/GA (BP:PVA/GA) hydrogels were investigated by FTIR, XRD, SEM, and antimicrobial tests. The durability of the functions was also examined by UV‐Vis spectroscopy, HPLC, MS, and antimicrobial tests. The concentrations of BP and GA in the BP:PVA/GA hydrogels affected the formation of the hydrogels as well as their structures. All BP:PVA/GA hydrogels showed antimicrobial abilities under UVA (365 nm) irradiation, and the effectiveness increased as the amounts of BP in the hydrogels increased. In particular, as‐prepared BP:PVA/GA hydrogels exhibited prominent durability in the photo‐induced antimicrobial ability. POLYM. ENG. SCI., 50:1780–1787, 2010. © 2010 Society of Plastics Engineers     

Pervaporation behavior of PVA membrane containing β‐cyclodextrin for separating xylene isomeric mixtures

To evaluate molecular recognition function of β‐cyclodextrin to xylene isomers, β‐CD polymer of branching chain extension (β‐CD‐EGDE) was synthesized by crosslinking β‐CD with ethylene glycol diglycidyl ether (EGDE). The pervaporation blend membranes of β‐CD‐EGDE/PVA were prepared by casting an aqueous solution of PVA and β‐CD polymer mixture, and the membranes were used for separation of p‐/m‐ and p‐/o‐xylene mixtures. It was observed that the pristine PVA membrane almost had no selectivity for xylene isomer mixtures. The PVA membrane incorporating β‐CD polymer had molecular recognition function, which selectively facilitated the transport of the xylene isomers. To ascertain pervaporation behavior, the sorption and desorption processes of the membrane in xylenes were investigated. The sorption result showed that the complex formation constant between β‐CDs and xylenes played a key role in swelling behavior. There was a significant difference between diffusion coefficients D and D⁰, calculated from the sorption and desorption measurements, respectively, indicating that the diffusivity selectivity in desorption stage may have remarkable effect on the total selectivity during pervaporation process. © 2012 American Institute of Chemical Engineers AIChE J, 59: 604–612, 2013     

Preparation and characterization of β‐cyclodextrin‐linked chitosan microparticles

Hydrophobically modified chitosan containing β‐cyclodextrin (CD) units was synthesized by using tosylated β‐CD. The final product was characterized by Fourier transform infrared (FTIR) spectroscopy, elemental analysis and TGA, and rheometry. The polymer bearing β‐CD moieties was used to obtain crosslinked microparticles by spray‐drying which could then be used in a controlled release system for drugs. FTIR confirmed the formation of an amide linkage between cyclodextrin and chitosan. As fluorescence spectroscopy demonstrated, hydrophobic microenvironments were formed by chitosan bearing cyclodextrin in solution at lower concentrations than for chitosan. Rheometry and FTIR showed the crosslinking of the new polymer using genipin, a molecule of natural origin. Microspheres (MS) obtained by spray‐drying showed narrow size distribution when β‐CD was grafted onto chitosan and ξ‐potential of MS was slightly lower although it remained positive. In conclusion, β‐CD linked chitosan polymer can be considered as a very promising controlled drug delivery system for drugs. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

Near‐Infrared Light‐Triggered Dual Drug Release Using Gold Nanorod‐Embedded Thermosensitive Nanogel‐Crosslinked Hydrogels

Gold nanorod (AuNR)‐embedded poly(N‐isopropylacrylamide) (PNIPAM) hydrogels offer the possibility of achieving near‐infrared (NIR) light‐triggered drug release. In addition, using nanoparticles as a crosslinker can enhance the mechanical properties of PNIPAM hydrogels, and nanoparticle‐crosslinked hydrogels provide an important approach for dual drug release. Here, NIR light‐triggered dual drug release using AuNR‐embedded thermosensitive nanogel‐crosslinked hydrogels is reported for the first time. Two kinds of drugs are encapsulated, one in the nanogel and the other in the hydrogel. The volume phase transition of the PNIPAM hydrogels is induced by NIR light by utilizing the photothermal effect of AuNRs. By changing the number of embedded AuNRs and the intensity of NIR light, the release rate and drug quantity can be adjusted for on‐demand release. Because of its NIR light‐triggering and nanoparticle‐crosslinking capabilities, AuNR‐embedded thermosensitive nanogel‐crosslinked hydrogels may expand the application scope of hydrogels and provide enhanced properties in their applications.     

Preparation of sodium alginate/poly(vinyl alcohol) blend microspheres for controlled release applications

Sodium alginate (NaAlg)/poly (vinyl alcohol) (PVA) blend microspheres (MS) were prepared by water-in-oil (w/o) emulsion method. These polymer microspheres were crosslinked with glutaraldehyde and loaded with metformin hydrochloride (MHC). The microspheres were characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and X-ray diffraction (XRD) analysis to confirm the molecular dispersion of the drug, thermal stability, morphological properties, and crystallinity of the polymer matrix before and after blending. SEM of the microspheres suggested the formation of microspheres in spherical structure. Drug release data were analyzed using an empirical equation to understand the nature of drug transport through polymeric matrices. The controlled release (CR) characteristics of the polymer matrices was investigated in pH 7.4 media and from the results it was obtained that the drug was released in controlled manner up to 10 h. The physico-chemical properties of the microspheres were studied by calculating drug entrapment efficiency and drug release kinetics. Percent of encapsulation efficiency (% EE) decreased with increase in crosslinking agent (GA) and PVA content in the microspheres. The optimum % EE (80%) was observed in case of MS containing 40% of PVA with 15% MHC. The release profiles indicate that the release of MHC decreases with increasing the PVA/NaAlg (w/w) and drug/polymer ratio. At the end of 10 h, the highest release of MHC was found to be 96% for MS containing PVA/NaAlg (40 : 60) and 15 wt % drug loaded. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

Electrostatic immobilization of cetylpyridinium chloride to poly(vinyl alcohol) hydrogels for the simple fabrication of wound dressings with the suppressed release of antibacterial agents

Polymeric systems for antibacterial wound dressings require chemical reactions or syntheses for attaching or incorporating antibacterial moieties into polymer backbones. However, these materials often fail to satisfy the basic requirements, such as easy and inexpensive synthesis. We speculated that a positively charged organic antibacterial agent would be attracted to the polar groups of poly(vinyl alcohol) (PVA) hydrogels and would show suppressed release. PVA hydrogels containing cetylpyridinium chloride (CPC) were prepared by γ irradiation. CPC was barely released from the hydrogels, probably because of electrostatic interactions, and was stable upon γ irradiation. The suppressed release of CPC conferred antibacterial activity against Escherichia coli to the surface of the hydrogels, whereas no inhibition zone was observed around the hydrogels. The CPC‐containing PVA hydrogels were easy to prepare and contained known and safe materials. The simplicity and safety of this procedure for achieving the suppressed release of antibacterial agents were advantages of these CPC‐containing PVA hydrogels. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40456.     

Synthesis and evaluation of sucrose‐containing polymeric hydrogels for oral drug delivery

Biodegradable and biocompatible copolymeric hydrogels based on sucrose acrylate, N‐vinyl‐2‐pyrrolidinone, and acrylic acid were designed and synthesized. Because of the growing importance of sugar‐based hydrogels as drug delivery systems, these new pH‐responsive sucrose‐containing copolymeric hydrogels were investigated for oral drug delivery. The sucrose acrylate monomer was synthesized and characterized. The copolymeric hydrogel was synthesized by free‐radical polymerization. Azobisisobutyronitrile (AIBN) was the free‐radical initiator employed and bismethyleneacrylamide (BIS) was the crosslinking agent used for hydrogel preparations. Homopolymeric vinyl pyrrolidone hydrogels were also prepared by the same technique. The hydrogels were characterized by differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. Equilibrium swelling studies were carried out in enzyme‐free simulated gastric and intestinal fluids (SGF and SIF, respectively). These results indicate the pH‐responsive nature of the hydrogels. The gels swelled more in SIF than in SGF. A model drug, propranolol hydrochloride (PPH), was entrapped in these gels and the in vitro release profiles were established separately in both enzyme‐free SGF and enzyme‐free SIF. The drug release was found to be faster in SIF. About 93 and 99% of the entrapped drug was released over a period of 24 h in SGF and SIF, respectively. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 84: 2597–2604, 2002     

Properties of hydrogels of atactic poly(vinyl alcohol)/NaCl/H2O system and their application to drug release

In order to prepare cost‐effective physically cross‐linked hydrogels including food salt sodium chloride, samples, were prepared with various concentrations of NaCl and respective atactic poly(vinyl alcohol) (a‐PVA), and were evaluated. It had been observed that hydrogels containing NaCl concentration (9–11 wt%) along with a‐PVA concentration 9–5% respectively exhibited higher melting points (91.5–95.1 °C). A higher melting point characterizes the hydrogel composition of a system like a‐PVA(7%)/NaCl(11%)/H₂O. The swelling degree of this hydrogel was found to be comparatively better at 37 °C than at any other temperature studied here. However, irregular Fickian swelling was found at this temperature. The UV light absorption maximum at 362–364 nm and minimum at 351 nm for this hydrogel had been found as evidence of physical cross‐linking. A drug, theophylline was loaded by solvent‐sorption and feed‐mixture dissolving methods. The feed‐mixture dissolving method is better than solvent sorption because of high drug loading, comparatively low fraction release rate and more sustained‐release of drug than that of solvent‐sorption. Theophylline was released twice as fast from the hydrogel after solvent‐sorption drug loading (3 h) than from that which used the feed‐mixture dissolving method (6.5 h). Theophylline‐loaded hydrogels of this system (feed‐mixture dissolving) were then prepared at high temperature (60 °C) thawing for 6 h followed by chilling at 0.4 °C for 3 h as one cycle. And the drug release behaviour and mass transfer were found almost the same as for chilling (24 h at 0.4 °C)–thawing (48 h at room temperature). Drug release behaviour was studied as apparently irregular Fickian diffusion (Higuchi Matrix Dissolution Model). © 2002 Society of Chemical Industry