3D-Printed Coating of Extended-Release Matrix Tablets: Effective Tool for Prevention of Alcohol-Induced Dose Dumping Effect

Tablets used for extended drug release commonly contain large amounts of drugs. The corresponding drug release mechanism thus has to be well-known and invariable under numerous conditions in order to prevent any uncontrolled drug release. Particularly important is the stability and invariability of the release mechanism in the presence of alcohol due to the possible occurrence of the dose dumping effect. The effect of 3D printing (3DP) coating on the drug release mechanism and the drug release rate was studied as a possible tool for the prevention of the alcohol-induced dose dumping effect. Three types of matrix tablets (hydrophilic, lipophilic, and hydrophilic-lipophilic) were prepared by the direct compression method and coated using 3DP. The commercial filament of polyvinyl alcohol (PVA) and the filament prepared from hypromellose by hot melt extrusion (HME) were used as coating materials. Both coating materials were characterized by SEM, DSC, Raman spectroscopy, and PXRD during particular stages of the processing/coating procedure. The dissolution behavior of the uncoated and coated tablets was studied in the strongly acidic (pH 1.2) and alcoholic (40% of ethanol) dissolution media. The dissolution tests in the alcoholic medium showed that the Affinisol coating was effective in preventing the dose dumping incidence. The dissolution tests in the acidic dissolution media showed that the Affinisol coating can also be useful for the delayed release of active substances.

Design and Application of Near-Infrared Nanomaterial-Liposome Hybrid Nanocarriers for Cancer Photothermal Therapy

Liposomes are attractive carriers for targeted and controlled drug delivery receiving increasing attention in cancer photothermal therapy. However, the field of creating near-infrared nanomaterial-liposome hybrid nanocarriers (NIRN-Lips) is relatively little understood. The hybrid nanocarriers combine the dual superiority of nanomaterials and liposomes, with more stable particles, enhanced photoluminescence, higher tumor permeability, better tumor-targeted drug delivery, stimulus-responsive drug release, and thus exhibiting better anti-tumor efficacy. Herein, this review covers the liposomes supported various types of near-infrared nanomaterials, including gold-based nanomaterials, carbon-based nanomaterials, and semiconductor quantum dots. Specifically, the NIRN-Lips are described in terms of their feature, synthesis, and drug-release mechanism. The design considerations of NIRN-Lips are highlighted. Further, we briefly introduced the photothermal conversion mechanism of NIRNs and the cell death mechanism induced by photothermal therapy. Subsequently, we provided a brief conclusion of NIRNs-Lips applied in cancer photothermal therapy. Finally, we discussed a synopsis of associated challenges and future perspectives for the applications of NIRN-Lips in cancer photothermal therapy.

Microsponge : An Overview

Microsponges are a revolutionary way of medication administration that has a number of advantages. The Microsponges drug delivery system is used to increase the performance of medications that are delivered orally, parenterally, or topically in a variety of conditions. Microsponge is a new technology for controlling medication release and delivering drugs to precise targets. Microsponge technology has been used in topical medicinal solutions to allow for regulated active drug release into the skin, lowering systemic exposure and reducing local cutaneous reactions to active pharmaceuticals. This review discusses the preparation procedures, evaluation methodologies, drug release mechanism, and physical characterization of Microsponges in relation to a Microsponges delivery system. Microsponges are used to deliver a pharmaceutical active component at a low dose while simultaneously improving stability, reducing adverse effects, and modifying drug release.

Effects of the Blending Ratio on the Design of Keratin/Poly(butylene succinate) Nanofibers for Drug Delivery Applications

In recent years there has been a growing interest in the use of proteins as biocompatible and environmentally friendly biomolecules for the design of wound healing and drug delivery systems. Keratin is a fascinating protein, obtainable from several keratinous biomasses such as wool, hair or nails, with intrinsic bioactive properties including stimulatory effects on wound repair and excellent carrier capability. In this work keratin/poly(butylene succinate) blend solutions with functional properties tunable by manipulating the polymer blending ratios were prepared by using 1,1,1,3,3,3-hexafluoroisopropanol as common solvent. Afterwards, these solutions doped with rhodamine B (RhB), were electrospun into blend mats and the drug release mechanism and kinetics as a function of blend composition was studied, in order to understand the potential of such membranes as drug delivery systems. The electrophoresis analysis carried out on keratin revealed that the solvent used does not degrade the protein. Moreover, all the blend solutions showed a non-Newtonian behavior, among which the Keratin/PBS 70/30 and 30/70 ones showed an amplified orientation ability of the polymer chains when subjected to a shear stress. Therefore, the resulting nanofibers showed thinner mean diameters and narrower diameter distributions compared to the Keratin/PBS 50/50 blend solution. The thermal stability and the mechanical properties of the blend electrospun mats improved by increasing the PBS content. Finally, the RhB release rate increased by increasing the keratin content of the mats and the drug diffused as drug-protein complex.

Excipients, drug release mechanism and physicochemical characterization methods of Solid lipid nanoparticles

From last thirty years, solid lipid nanoparticles (SLNs) gain much importance as drug delivery vehicle for enhanced delivery of the drugs, proteins, nutraceuticals and cosmetics. SLNs defined as a submicron size range nanoparticle with below 1000 nm and are mainly composed of lipids and surfactants, capable of incorporating both lipophilic and hydrophilic drugs. SLNs also used as controlled systems, targeted delivery and altered therapeutic efficacy purpose. A wide variety of methods such as double emulsion, solvent evaporation, ultra sonication, high-pressure homogenization and microemulsion used for SLNs production. This review provides the significance of SLNs in drug delivery with highlighting on selection of excipients, drug release mechanism, principles and limitations associated with their physicochemical and surface morphological characterization. Keywords: Solid lipid nanoparticles, enhanced delivery, preparation, characterization, application.

A Drug Release Mechanism Controlled by Hydrophobic/Hydrophilic Balance of the Matrix. Theoretical and Experimental Perspectives

Controlled drug release is a promising pathway of biomedicine, meant to suppress side effects with the aim of increasing patient s comfort. A route to achieve this goal represents the encapsulation of drugs into matrixes, capable to develop physical forces, which further can control the drugs release. To this purpose, mathematical modeling is an important tool, which offers the possibility to understand the drug release mechanisms and to further design new performant systems. In this paper, a theoretical model for drug release from an amphiphilic matrix is presented. This is achieved using a conservation multifractal law of probability density followed by validation of the model. Moreover, because non-steroidal anti-inflammatory drugs (NSAIDs), such as diclofenac, are widely used in endometriosis as painkillers for dysmenorrhea management or Asherman syndrome for reducing the endometrial inflammation, some implications of our model for drug delivery systems applied in the field of gynecology have been discussed.

Techniques of Mucilage and Gum Modification and their Effect on Hydrophilicity and Drug Release

Aim: The manuscript aims to describe the techniques of modification of gums and mucilages and their effect on hydrophilicity and drug release. Discussion: The interest is increased in the fields of polymers which is obtained from natural origin and used in the preparation of pharmaceuticals. Mucilage and gum are natural materials, widely used in the preparation of novel dosage form and conventional dosage form. They are used in the pharmaceutical industry for various purposes like suspending, emulsifying, bio-adhesive, binding, matrix-forming, extended release and controlled release agent. Gum and mucilage are biodegradable, less toxic, cheap and easily available. Moreover, mucilage and gum can be changed to acquire tailored materials for the delivery of drugs and allow them to compete with commercially available synthetic products. These polysaccharides have unique swellability in an aqueous medium that can exert a retardant effect on drug release or act as a super disintegrant, depending on the concentration utilized in the preparation. Drug release mechanism from hydrophilic matrices consisting of gums and mucilages is based on solvent penetration-induced polymer relaxation, diffusion of entrapped drug followed by degradation or erosion of the matrix. Conclusion: The present manuscript highlight the advantages, modifications of gum and mucilage, their effects on hydrophilicity and drug release as well as aspects of the natural gums which can be assumed to be bifunctional excipient because of their concentration-dependent effect on drug release and their high degree of swellability.

5-Fluorouracil Release from Chitosan-Based Matrix.Experimental and Theoretical Aspects

A series of four drug release formulations based on 5-fluorouracil encapsulated into a chitosan-based matrix were prepared by in situ hydrogelation with 3,7-dimethyl-2,6-octadienal. The formulations were investigated from structural and morphological aspects by FTIR spectroscopy, polarized light microscopy and scanning electron microscopy. It was established that 5-fluorouracil was anchored into the matrix as crystals, whose dimension varied as a function of the crosslinking density. The in vitro drug release simulated into a media mimicking the physiological environment revealed a progressive release of the 5-fluorouracil, in close interdependence with the crosslinking density. In the context of Pharmacokinetics behavioral analysis, a new mathematical procedure for describing drug release dynamics in polymer-drug complex system is proposed. Assuming that the dynamics of polymer-drug system�s structural units take place on continuous and nondifferentiable curves (multifractal curves), we show that in a one-dimensional hydrodynamic formalism of multifractal variables the drug release mechanism (Fickian diffusion, non-Fickian diffusion, etc) are given through synchronous dynamics at a differentiable and non-differentiable scale resolutions. Finally, the model is confirmed by the empirical data.

A mesostructured hybrid CTA–silica carrier for curcumin delivery

Curcumin is a natural active principle with antioxidant, antibacterial and anti-inflammatory properties. Its use is limited by a low water solubility and fast degradation rate, which hinder its bioavailability. To overcome this problem, curcumin can be delivered through a carrier, which protects the drug molecule and enhances its pharmacological effects. The present work proposes a simple one-pot sol–gel synthesis to obtain a hybrid carrier for curcumin delivery. The hybrid consists of a mesostructured matrix of amorphous silica, which stabilizes the carrier, and hexadecyltrimethylammonium (CTA), a surfactant where curcumin is dissolved to increase its water solubility. The carrier was characterized in terms of morphology (FESEM), physicochemical properties (XRD, FTIR, UV spectroscopy) and release capability in pseudo-physiological solutions. Results show that curcumin molecules were entrapped, for the first time, in a silica-surfactant mesostructured hybrid carrier. The hybrid carrier successfully released curcumin in artificial sweat and in a phosphate buffer saline solution, so confirming its efficacy in increasing curcumin water solubility. The proposed drug release mechanism relies on the degradation of the carrier, which involves the concurrent release of silicon. This suggests strong potentialities for topical administration applications, since curcumin is effective against many dermal diseases while silicon is beneficial to the skin.

Encapsulation for Cancer Therapy

The current rapid advancement of numerous nanotechnology tools is being employed in treatment of many terminal diseases such as cancer. Nanocapsules (NCs) containing an anti-cancer drug offer a very promising alternative to conventional treatments, mostly due to their targeted delivery and precise action, and thereby they can be used in distinct applications: as biosensors or in medical imaging, allowing for cancer detection as well as agents/carriers in targeted drug delivery. The possibility of using different systems—inorganic nanoparticles, dendrimers, proteins, polymeric micelles, liposomes, carbon nanotubes (CNTs), quantum dots (QDs), biopolymeric nanoparticles and their combinations—offers multiple benefits to early cancer detection as well as controlled drug delivery to specific locations. This review focused on the key and recent progress in the encapsulation of anticancer drugs that include methods of preparation, drug loading and drug release mechanism on the presented nanosystems. Furthermore, the future directions in applications of various nanoparticles are highlighted.