Applications In Pharmaceutical Technology Research Articles

Influence of HA on Release Process of Anionic and Cationic API Incorporated into Hydrophilic Gel.

The properties of sodium hyaluronate (HA), such as hygroscopicity, flexibility, the ability to form hydrogels, as well as biocompatibility and biodegradability, are beneficial for the applications in pharmaceutical technology, cosmetics industry, and aesthetic medicine. The aim of this study was to prepare HA-based hydrogels doped with active pharmaceutical ingredient (API): a cationic drug-lidocaine hydrochloride or anionic drug-sodium. The interaction between the carrier and the implemented active pharmaceutical substances was evaluated in prepared systems by applying viscometric measurements, performing release tests of the drug from the obtained formulations, and carrying out FTIR and DSC. The data from release studies were analyzed using the zero-, first-, and second-order kinetics and Higuchi, Korsmeyer-Peppas, and Hixon-Crowell models. The respective kinetic parameters: the release rate constants, the half-release time and, in the case of the Korsmeyer-Peppas equation, the n parameter were calculated. The variability between the obtained release profiles was studied by calculating the difference (f1) and the similarity factor (f2) as well as employing statistical methods. It was revealed that the incorporation of the drugs resulted in an increase in the viscosity of the hydrogels in comparison to the respective drug-free preparations. The dissolution study showed that not entire amount of the added drug was released from the formulation, suggesting an interaction between the carrier and the drug. The FTIR and DSC studies confirmed the bond formation between HA and both medicinal substances.

Alginates Combined with Natural Polymers as Valuable Drug Delivery Platforms.

Alginates (ALG) have been used in biomedical and pharmaceutical technologies for decades. ALG are natural polymers occurring in brown algae and feature multiple advantages, including biocompatibility, low toxicity and mucoadhesiveness. Moreover, ALG demonstrate biological activities per se, including anti-hyperlipidemic, antimicrobial, anti-reflux, immunomodulatory or anti-inflammatory activities. ALG are characterized by gelling ability, one of the most frequently utilized properties in the drug form design. ALG have numerous applications in pharmaceutical technology that include micro- and nanoparticles, tablets, mucoadhesive dosage forms, wound dressings and films. However, there are some shortcomings, which impede the development of modified-release dosage forms or formulations with adequate mechanical strength based on pure ALG. Other natural polymers combined with ALG create great potential as drug carriers, improving limitations of ALG matrices. Therefore, in this paper, ALG blends with pectins, chitosan, gelatin, and carrageenans were critically reviewed.

A Comprehensive Review on Preparation, Evaluation and Applications of Deformable Liposomes

Elastic or deformable liposomes are phospholipid-based vesicular drug delivery systems that help improve the delivery of therapeutic agents through the intact skin membrane due to their deformable characteristics that overcome the problems of conventional liposomes. In the present review, different types of deformable liposomes such as transfersomes, ethosomes, menthosomes, invasomes and transethosome are studied, and their mechanism of action, characterization, preparation methods, and applications in pharmaceutical technology through topical, transdermal, nasal and oral routes for effective drug delivery are compared for their potential transdermal delivery of poorly permeable drugs. Due to the deformable characteristics of these vehicles, it resulted in modulation of increased drug encapsulation efficiency, permeation and penetration of the drug into or through the skin membrane and are found to be more effective than conventional drug delivery systems. So deformable liposomes can, therefore, be considered as a promising way of delivering the drugs transdermally.

Polyglycerol Hyperbranched Polyesters: Synthesis, Properties and Pharmaceutical and Biomedical Applications.

In a century when environmental pollution is a major issue, polymers issued from bio-based monomers have gained important interest, as they are expected to be environment-friendly, and biocompatible, with non-toxic degradation products. In parallel, hyperbranched polymers have emerged as an easily accessible alternative to dendrimers with numerous potential applications. Glycerol (Gly) is a natural, low-cost, trifunctional monomer, with a production expected to grow significantly, and thus an excellent candidate for the synthesis of hyperbranched polyesters for pharmaceutical and biomedical applications. In the present article, we review the synthesis, properties, and applications of glycerol polyesters of aliphatic dicarboxylic acids (from succinic to sebacic acids) as well as the copolymers of glycerol or hyperbranched polyglycerol with poly(lactic acid) and poly(ε-caprolactone). Emphasis was given to summarize the synthetic procedures (monomer molar ratio, used catalysts, temperatures, etc.,) and their effect on the molecular weight, solubility, and thermal and mechanical properties of the prepared hyperbranched polymers. Their applications in pharmaceutical technology as drug carries and in biomedical applications focusing on regenerative medicine are highlighted.

Elastic liposomes as novel carriers: recent advances in drug delivery.

Elastic liposomes (EL) are some of the most versatile deformable vesicular carriers that comprise physiologically biocompatible lipids and surfactants for the delivery of numerous challenging molecules and have marked advantages over other colloidal systems. They have been investigated for a wide range of applications in pharmaceutical technology through topical, transdermal, nasal, and oral routes for efficient and effective drug delivery. Increased drug encapsulation efficiency, enhanced drug permeation and penetration into or across the skin, and ultradeformability have led to widespread interest in ELs to modulate drug release, permeation, and drug action more efficiently than conventional drug-release vehicles. This review provides insights into the versatile role that ELs play in the delivery of numerous drugs and biomolecules by improving drug release, permeation, and penetration across the skin as well as stability. Furthermore, it provides future directions that should ensure the widespread use of ELs across all medical fields.

Use of Pseudoboehmite Nanoparticles for Drug Delivery System of Glucantime®

Recently, the incidence of American Cutaneous Leishmaniasis (ACL) has been grown in Latin America, especially in Brazil, where from 1980 to 2005, 605,062 cases were recorded. The drug glucantime®, whose active principle is the meglumine antimoniate (or meglumine antimonate) is used in the treatment of leishmaniasis. Its toxicity is due mainly to the presence of antimony in its structure. Therefore, it is crucial to determine the safe dose levels of this drug in the treatment. Drug delivery systems have been currently the focus of many studies due to its effectiveness in treating diseases proved to be superior compared to conventional methods. Drug delivery systems can avoid overdosing by decreasing the amount of drug intake, which results in a better therapeutic effect in addition to reducing the risks of plasma concentration reaching toxic levels. Synthetic nanomaterials have been receiving great attention due to their potential applications in pharmaceutical technology as well as the possibility of controlling their particle size and composition, which allows a better performance in drug release. Pseudoboehmite is a synthetic aluminum compound precursor of alumina [1] and a polymorph of boehmite, with active groups in its structure [2], making it an excellent adsorbent material. In this work, pseudoboehmite was prepared by using the sol-gel process for being used as an excipient. The incorporation of pseudoboehmite in glucantime® was performed in the processing of tablets. Both pseudoboehmite and the tablets were characterized via X-ray diffraction (XRD), differential thermal analysis (DTA), thermogravimetric analysis (TG), and scanning electron microscopy (SEM) using secondary electron detector and EDS detector. The release profile was obtained by UV/Vis spectroscopy for in vitro simulation. No reaction between the drug and the excipient was observed.

Effect of ethyl acetate fraction of urucum extract on cell viability of peripheral blood mononuclear cells and antimicrobial activity in human pathogenic bacteria.

Effect of ethyl acetate fraction of urucum extract on cell viability of peripheral blood mononuclear cells and antimicrobial activity in human pathogenic bacteria.

A novel process for coating of silica aerogel microspheres for controlled drug release applications

Aerogels are nanoporous materials with an open-pore structure and high specific surface area. Because of their outstanding properties they have been investigated in immense fields of applications like novel insulation materials, catalysts and catalysts carrier, optics, waste treatment and drug delivery systems. However, the limitation of aerogels (specially hydrophilic ones) in a number of applications is their open-pore structure, allowing the penetration of liquids therein resulting in destruction of their textural properties. Applying a polymeric coating layer on aerogels surface can be a solution for this problem and can open a wide window of new applications for aerogels, especially in pharmaceutical industry. This work suggests a novel process for coating of aerogels with polymeric materials using spouted bed technology. Firstly, spherical silica aerogel particles with a high surface area up to 1100m2/g and particles diameter ranging from 200μm to few millimetres were produced. Then, the aerogel particles were loaded with a model drug (Ibuprofen) by adsorption from supercritical CO2 phase. The loaded aerogel particles were coated with different polymeric materials in a slit-shaped spouted fluidized bed with two horizontal gas inlets and adjustable gas supply. The corresponding polymers were sprayed as an aqueous suspension or as melts. The process conditions for coating (coating material, fluidization air flow rate, temperature, etc.) were optimized accordingly. The physical, mechanical, structural and release properties of the resulting formulations were evaluated. This technology allows to provide a specific release mechanism of pharmaceuticals (thermal, pH-sensitive or enzyme triggered release) from aerogels and to broaden aerogel applications in pharmaceutical technology.

Laboratory SWAXS for applications in pharmaceutical technology

Laboratory SWAXS for applications in pharmaceutical technology

The Role of Chitosan in Drug Delivery

Chitosan, obtained by deacetylation of chitin, is a natural, hydrophilic, nontoxic, biocompatible, and biodegradable polysaccharide suitable for applications in pharmaceutical technology. Its role in drug delivery systems was examined by considering the chemical and biologic properties of the polymer. Chitosan is a nonbranched homopolymer formed by β-(1,4)-linked glucosamine units; hydroxyls and the amino groups are substrates for chemical modifications aimed at obtaining suitable materials for different purposes. Chitosan is soluble at acidic pH, forming gels; hydrogels are also formed in the presence of negatively charged drugs or polyanions, and represent a sustained drug release form. The bioadhesive nature of chitosan can be attributed to the same type of ionic interactions with mucosal membrane components. Mucoadhesive formulations have been developed for ocular, nasal, buccal, gastrointestinal, and vaginal drug administration. Chitosan is able to promote transmucosal absorption of small polar drugs, including peptides, inducing a transient opening of the tight junctions of the cell membrane. Due to its polymeric nature, chitosan has been widely investigated for a variety of microparticulate pharmaceutical forms. Chitosan is also a candidate for potential applications in the delivery of radiopharmaceuticals, genes and peptides.

Use of percolation theory to interpret water uptake, disintegration time and intrinsic dissolution rate of tablets consisting of binary mixtures

Percolation theory represents a novel powerful concept which covers a wide range of applications in pharmaceutical technology. In the present work the tablets used consist of StaRX1500® as a disintegrant and of caffeine as a model drug. The disintegrant content of the compacts is varied from 0 to 90% (w/w). The disintegration time tD, the kinetic constant of water uptake K and the intrinsic dissolution rate J are determined using appropriate methods.Plotting the results obtained as a function of the concentration of the disintegrant in percent (v/v), the resulting curves show an interesting section around 10% (v/v) StaRX1500 where the kinetic constant of water uptake K and the intrinsic dissolution rate J pass through maximum values and the disintegration time tD goes through a minimum value. Based on these observations it is evident that the concentration p of StaRX1500 reaches a critical value p∗(1) where the characteristics of the binary system change clearly. By plotting the whole curves in a log-log scale, three linear sections can be distinguished clearly. Therefore a second critical concentration p∗(2) is obtained in addition to the one described before.The critical concentration p∗(1) corresponds to the first percolation threshold pc1. For concentrations p < pc1 only finite clusters of StaRX1500, causing a positive influence on the disintegration process, exist in the tablets. Thus the isolated clusters within the pore structure of the more lipophilic caffeine increase the wettability of the porous system. For cocentrations p > pc1 an infinite cluster of StaRX1500 percolates through the compact, causing now a slower disintegration. The reason for the reducing effect lies in th fact that the pores start to close by the swelling of StaRX1500. Thus the entrance of water into the compact will be hindered as a function of the amount of disintegrant in the tablet. It can be assumed that the critical concentration p∗(2) corresponds to the upper percolation threshold pc2. Thus for concentrations of StaRX1500 above pc2 the caffeine is present as isolated clusters.

Optimisation in pharmaceutical sciences

Optimisation means finding the best possible value of a dependent variable by varying certain independent variables. Several optimisation techniques are discussed and their applications in pharmaceutical technology, analysis, clinical chemistry and medicinal chemistry are critically evaluated.