[Modern topical drugs-new developments in galenics and pharmacology]. / Moderne topische Arzneimittel ­ neue Entwicklungen in Galenik und Pharmakologie.

The importance of topically applied pharmaceuticals, especially for the treatment of dermatological diseases, is still essential. Thanks to detailed knowledge of the organisation and function of the physicochemical barrier of the skin, new galenic concepts have increasingly been developed to market maturity in recent years. Colloidal drug carrier systems in particular, but also targeted physicochemical modifications of matrices are used to optimise the cutaneous bioavailability of topically applied drugs. In addition, new molecules are increasingly becoming available for the development of these preparations or drugs known from systemic therapy are being formulated into topicals. Against this background, dermatopharmacology is also developing more and more into a highly specialised science in this area, which is producing innovative concepts for the therapy of special indications. In addition to the classic small-molecule drugs, biotechnological molecules are increasingly finding their way into application, so that a modern age of dermatopharmacology has dawned, which will open up previously unimagined possibilities for topical therapy now and in the coming years.

Exploring Synthesis Strategies and Interactions between MOFs and Drugs for Controlled Drug Loading and Release, Characterizing Interactions through Advanced Techniques.

This study explores various aspects of Metal-Organic Frameworks (MOFs), focusing on synthesis techniques to adjust pore size and key ligands and metals for crafting carrier MOFs. It investigates MOF-drug interactions, including hydrogen bonding, van der Waals, and electrostatic interactions, along with kinetic studies. The multifaceted applications of MOFs in drug delivery systems are elucidated. The morphology and structure of MOFs are intricately linked to synthesis methodology, impacting attributes like crystallinity, porosity, and surface area. Hydrothermal synthesis yields MOFs with high crystallinity, suitable for catalytic applications, while solvothermal synthesis generates MOFs with increased porosity, ideal for gas and liquid adsorption. Understanding MOF-drug interactions is crucial for optimizing drug delivery, affecting charge capacity, stability, and therapeutic efficacy. Kinetic studies determine drug release rates and uniformity, vital for controlled drug delivery. Overall, comprehending drug-MOF interactions and kinetics is essential for developing effective and controllable drug delivery systems.

Study of folate-based carbon nanotube drug delivery systems targeted to folate receptor α by molecular dynamic simulations.

We designed targeted drug delivery systems containing folate (FOL), the functionalized carbon nanotube (f-CNT) and doxorubicin (DOX), and studied the targeting properties of folate, f-CNT-FOL and DOX/f-CNT-FOL to folate receptor α (FRα). Folate was actively targeted to FRα in molecular dynamics simulations, and the dynamic process, effect of folate receptor evolution, and characteristics were analyzed. On this basis, the f-CNT-FOL and DOX/f-CNT-FOL nano-drug-carrier systems were designed, and the drug delivery process targeted to FRα was studied by 4 times MD simulations. The system evolution and detailed interactions of f-CNT-FOL and DOX/f-CNT-FOL with FRα residues were examined. We found that though the connection of CNT with the FOL could decrease the insertion depth of the pterin of FOL into the pocket of FRα, the loading of drug molecules could reduce this effect. Representative snapshots from the MD simulations were analyzed, showing that the location of DOX on the surface of CNT was constantly changed during the MD simulation, but the surface of the four rings of DOX were almost always parallel to the surface of CNT. The RMSD and RMSF were used to further analyze. The results may provide new insights for the design of novel targeted nano-drug-delivery systems.

Current outlook on radionuclide delivery systems: from design consideration to translation into clinics.

Radiopharmaceuticals have proven to be effective agents, since they can be successfully applied for both diagnostics and therapy. Effective application of relevant radionuclides in pre-clinical and clinical studies depends on the choice of a sufficient delivery platform. Herein, we provide a comprehensive review on the most relevant aspects in radionuclide delivery using the most employed carrier systems, including, (i) monoclonal antibodies and their fragments, (ii) organic and (iii) inorganic nanoparticles, and (iv) microspheres. This review offers an extensive analysis of radionuclide delivery systems, the approaches of their modification and radiolabeling strategies with the further prospects of their implementation in multimodal imaging and disease curing. Finally, the comparative outlook on the carriers and radionuclide choice, as well as on the targeting efficiency of the developed systems is discussed.

A QCM-based assay of drug content in Eudragit RS 100-based delivery systems.

A specific version of the quartz crystal microbalance method has been proposed for quantitative evaluation of drug content in polymeric drug carrier systems. In this study, ammonio methacrylate copolymer (type B) microparticles and their standard solutions have been prepared and loaded with set amounts of the medications diltiazem (base) and lidocaine. The analytes have been segregatim deposited on the surface of the resonator and the drug content in them has been derived from the downshift of the resonance frequency produced by irreversible interaction of the drug molecules with irradiating hydrochloric gas. The obtained results have been statistically processed on a number of samples and have been found to exhibit excellent coherence to set theoretical values. As an alternative, the conventional pharmacopoeial UV-Vis spectral method has also been separately applied to studied samples, revealing worsened performance in the case of lidocaine due to polymer matrix interference. Thus the universality of the QCM method has been proved to add to its versatility and precision. The method appears to be readily applicable to the routine pharmaceutical quantity control of bulk and multiparticulate drug forms.

Radiopharmaceutical enhancement by drug delivery systems: A review.

INTRODUCTION: Drug delivery systems are entities designed to alter the biological behaviour of the pharmaceutical active ingredients that they carry in order to afford more beneficial biodistribution and safety profiles. Many problems currently faced by the field of nuclear medicine (e.g. developing new theranostic agents, utilizing multimodal imaging platforms and providing targeted delivery) can be facilitated by applying drug delivery systems to radiopharmaceuticals that have been proven successful in other medical fields. This review describes the advancements being made towards this goal. AREAS COVERED: All aspects of drug delivery systems (liposomes, nanoparticles, microspheres) in the field of nuclear medicine are discussed. Only systems with foreseen or confirmed clinical applications in nuclear medicine are discussed, not instances where nuclear imaging is merely a tool to evaluate the biodistribution of novel delivery technologies. CONCLUSION: Great advancements have been made with the development of novel systems incorporating nuclear entities in drug delivery systems, with the possibility of reshaping the nuclear medicine landscape. Nonetheless, translation from preclinical evaluations to clinical use is lacking and serious investment needs to be made towards this goal.

Recent Developments in Controlled Release of Antibiotics.

Traditional use of antibiotics through injection or oral ingestion has many disadvantages, such as detrimental side effects in the host, less effectiveness, high and repeated doses, and development of drug resistance. For prevention and treatment of implant-associated infections, the continuous local delivery of antibiotics is required. Thus, there is a strong demand for the development of drug carrier systems to control the release of antibiotics in a moderate manner over an appropriate timescale. This review summarizes the carrier platforms used for the loading of antibiotics, and highlights their drug release behaviors as well as in vitro and in vivo antibacterial properties.

Radiolabeling of new generation magnetic poly(HEMA-MAPA) nanoparticles with (131) I and preliminary investigation of its radiopharmaceutical potential using albino Wistar rats.

In this study, N-methacryloyl-l-phenylalanine (MAPA) containing poly(2-hydroxyethylmethacrylate) (HEMA)-based magnetic poly(HEMA-MAPA) nanobeads [mag-poly(HEMA-MAPA)] were radiolabeled with (131) I [(131) I-mag-poly(HEMA-MAPA)], and the radiopharmaceutical potential of (131) I-mag-poly(HEMA-MAPA) was investigated. Quality control studies were carried out by radiochromatographic method to be sure that (131) I binded to mag-poly(HEMA-MAPA) efficiently. In this sense, binding yield of (131) I-mag-poly(HEMA-MAPA) was found to be about 95-100%. In addition to this, optimum radiodination conditions for (131) I-mag-poly(HEMA-MAPA) were determined by thin-layer radiochromatography studies. In addition to thin-layer radiochromatography studies, lipophilicity (partition coefficient) and stability studies for (131) I-mag-poly(HEMA-MAPA) were realized. It was determined that lipophilicities of mag-poly(HEMA-MAPA) and (131) I-mag-poly(HEMA-MAPA) were 0.12 ± 0.01 and 1.79 ± 0.76 according to ACD/logP algorithm program, respectively. Stability of the radiolabeled compound was investigated in time intervals given as 0, 30, 60, 180, and 1440 min. It was found that (131) I-mag-poly(HEMA-MAPA) existed as a stable complex in rat serum within 60 min. After that, biodistribution and scintigraphy studies were carried out by using albino Wistar rats. It was determined that the most important (131) I activity uptake was observed in the breast, the ovary, and the pancreas. Scintigraphy studies well supported biodistribution results.