HPMC- A Marvel Polymer for Pharmaceutical Industry-Patent review

: At the present time, designing of defined release dosage forms, either controlled, sustained, modified, are gaining much importance. For the development of such delivery systems, proper blend of polymers is required, so that drug release occurs by polymer erosion, swelling, diffusion/dissolution. HPMC (hydroxypropyl methyl cellulose) is the most commonly used cellulosic polymer available in various grades to develop such types of systems. Depending upon the molecular weight and viscosity chosen, it can be applied for emulsification, adhesion, bonding, thickening, suspension, film forming and gelation. It consists of polymeric units linked together, which retain water, thereby acting as an excellent hydrophilic gel-forming polymer. It generally hydrates on the outer surface to form a gelatinous layer. It swells, expands upon contact with water and releases the drug in a predetermined manner initially and then forms a viscous gel to control the release further. The objective of the present review is to overview the recent patents and articles of HPMC, its properties, grades and its use in various drug delivery systems and as a binder, dispersing agent, bioavailability enhancer and as capsule forming material have been identified and reviewed.

Assessment of biosafety and toxicity of hydrophilic gel for implantation in experimental in vitro and in vivo models

Background: The assessment of biosafety of pharmacologically active substances is crucial for determining the feasibility of their medical use. There are controversial issues regarding the use of substances of different origins as implants. Methods: We have conducted the comprehensive studies to determine the in vivo toxicity and in vitro genotoxicity of new generation of hydrophilic gel for implantation (production name of the substance "Activegel") to detail its characteristics and assess its biosafety. Results: In vivo studies have shown the absence of clinical manifestations of intoxication in animals and no abnormalities in their physiological condition, general and biochemical blood tests. Evaluation of the site of the gel application showed no inflammatory reaction and evidenced on normal state of tissues of animal skin. The results of the genotoxicity test indicated that the gel did not affect the parameters of DNA comets and, accordingly, had no genotoxic effect on human peripheral blood lymphocytes. When studying the effect of the gel on malignantly transformed cells in vitro, it was found that the gel for implantation did not change the proliferative activity and viability of human breast cancer cells. Conclusions: Comprehensive in vitro and in vivo study using various experimental model systems showed that the hydrophilic gel for implantation "Activegel" is non-toxic.

Medical treatment of polymeric cerebral granulomatous reactions following endovascular procedures

BackgroundEndovascular procedures are standard of care for an increasing range of cerebrovascular diseases. Many endovascular devices contain plastic and are coated with a hydrophilic polymer which has been rarely described to embolize, resulting in distal granulomatous inflammatory lesions within the vascular territory.MethodsWe reviewed three cases of cerebral granulomatous reactions that occurred after endovascular intervention for internal carotid aneurysms. The patient procedure details, presentation, relevant investigations, and treatment course are described. We also provide a literature review on endovascular granulomatous reactions.ResultsThese three cases represent the largest biopsy proven series of cerebral granulomatosis following endovascular intervention. We highlight the variable clinical presentation, with two of the three cases having an unusually delayed onset of up to 4 years following the intervention. We show the characteristic histological findings of granulomatous lesions with foreign body material consistent with a type IV reaction, radiological abnormalities of enhancing lesions within the vascular territory of the intervention, and the requirement of prolonged immunosuppression for maintenance of clinical remission, with two of the three patients requiring a corticosteroid sparing agent. In comparison with the available literature, in addition to hydrophilic gel polymer, we discuss that plastic from the lining of the envoy catheter may be a source of embolic material. We also discuss the recommendations of the Food and Drug Administration and the implementation of novel biomaterials for the prevention of these reactions in the future.ConclusionsThere is a need for increased awareness of this severe complication of cerebral endovascular procedures and further longitudinal studies of its prevalence, optimal management and preventative measures.

Multifunctional glycerol/citric acid crosslinked polymer hydrophilic gel with absorptive and reducing properties

Multifunctional hydrogel based on glycerol/citric acid presents absorptive and reducing capacities, affording a hybrid gel containing AgNPs in the matrix.

Bipolymeric Pectin Millibeads Doped with Functional Polymers as Matrices for the Controlled and Targeted Release of Mesalazine

Targeted drug delivery systems are a very convenient method of treating inflammatory bowel disease. The properties of pectin make this biopolymer a suitable drug carrier. These properties allow pectin to overcome the diverse environment of the digestive tract and deliver the drug to the large intestine. This investigation proposed bipolymeric formulations consisting of the natural polymer pectin and a synthetic polymer containing the drug 5-aminosalicylic acid. Pectin beads were prepared via ionotropic gelation involving the interaction between the hydrophilic gel and calcium ions. The obtained formulations consisted of natural polymer, 5-aminosalicylic acid (5-ASA) and one of the synthetic polymers, such as polyacrylic acid, polyvinylpyrrolidone, polyethylene glycol or aristoflex. The release of the drug was carried out employing a basket apparatus (USP 1). The acceptor fluid was pH = 7.4 buffer with added enzyme pectinase to reflect the colon environment. The amount of the released drug was determined using UV-Vis spectrophotometry at a wavelength of λ = 330 nm. The kinetics of the drug dissolution revealed that none of the employed models was appropriate to describe the release process. A kinetic analysis of the release profile during two release stages was carried out. The fastest drug release occurred during the first stage from a formulation containing pectin and polyethylene glycol. However, according to the applied kinetic models, the dissolution of 5-ASA was rather high in the formulation without the synthetic polymer during the second stage. Depending on the formulation, 68–77% of 5-ASA was released in an 8-hour time period. The FTIR and DSC results showed that there was no interaction between the drug and the polymers, but interactions between pectin and synthetic polymers were found.

Topical Administration of Cannabidiol: Influence of Vehicle-Related Aspects on Skin Permeation Process

Cannabidiol (CBD) is a non-psychoactive cannabinoid isolated from Cannabis sativa which, given its claimed beneficial properties and therapeutic potential, has lately aroused considerable attention from the scientific community. Starting from the little literature evidence, the main purpose of this study was to investigate the topical administration of CBD, with particular focus on the influence of vehicle-related aspects on the skin permeation process. This could provide useful information for the design of suitable drug delivery systems which could be used in developing topical medicines and cosmetics. In vitro human skin permeation studies were conducted using modified Franz diffusion cells to compare the performance of four solutions and two semisolid formulations. The Hildebrand solubility parameter was used to better understand the thermodynamic aspects implied in the partitioning process of the cannabinoid compound into the skin. It was interestingly found that a hydrophilic gel, mostly consisting of propylene glycol (79%, w/w), can be an optimal choice for the topical administration of CBD. Moreover, the feasibility of the preparation of CBD-loaded (trans)dermal patches, made with new printing technology, was also demonstrated.

Influence of Acid Etching and Universal Adhesives on the Bond Strength to Dentin

The purpose of this study was to evaluate the influence of the application mode of three universal adhesive systems on interfacial physical properties of indirect composite restorations adhesively cemented to dentin cavities. Seventy-eight bovine lower incisors were selected and a slice of dentin (thickness: 2 mm) between the buccal surface and pulp chamber was obtained for each tooth. Conical cavities were made on this surface. The internal walls of the cavities were then coated with a hydrophilic gel, filled with composite resin and photopolymerized. The dentin/cone sets were divided into 6 groups (n=10) according to type of universal adhesive (TETRI: Tetric N Bond, FUT: Futura Bond U, SBU: Single Bond Universal) and acid etching on dentin (A: with acid etching; WA: without acid etching). The acid etching and the adhesive systems were applied to the surface of the dentin. All composite resin cones were sandblasted (Al2O3, 20 s) and silanized. After surface treatment, the cones were cemented (RelyX Ultimate) into the dentin cavity and photopolymerized. After thermocycling (10,000 cycles), samples were submitted to marginal adaptation analysis (using caries detector dye), push-out test (0.5 mm/min), and failure mode analysis. Additional samples were prepared for nanoleakage analysis (SEM). The data (MPa) were analyzed by two-way ANOVA and Tukey’s post-test (5%). The groups in which the dentin was acid etched showed significantly lower bond strength values in the push-out test (p<0.01). Dentin acid etching significantly reduced the bond strength between universal adhesive systems and dentin in indirect restorative procedures.