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•Active targeting to reduce cytotoxicity of paclitaxel towards healthy cells.•The amount of paclitaxel for incorporation in the bilayer of liposome is limited.•Paclitaxel loading in ...core and bilayer sections of liposome shows sustained release.•Surface functionalization of micelle, liposome, and cubosome should be considered.
The diterpenoid molecule paclitaxel (PTX), extracted from the Western yew tree, Taxus brevifolia, is a promising anticancer drug specifically in clinical use for ovarian and breast cancers. However, its wider use is hampered by adverse effects and emerging resistance in cancer cells. Micelles, liposomes, cubosomes, and lipid nanoparticles (LNPs) have the potential to reduce or even remove complications associated with the use of PTX. Herein, we provide an overview of micro- and nanoformulations of PTX based on micelles, liposomes, cubosomes and LNPs to improve the therapeutic effects of this drug both in vitro and in vivo.
The anti-adhesion, anti-growth and the anti-penetration of bacteria, specifically multidrug-resistant bacteria, should be taken into consideration when designing promising wound dressings for ...infected wounds such as diabetic foot ulcers. Wound dressings composed of natural polymeric nanofibers such as functionalized cellulose, chitosan, alginate, hyaluronic acid, dextrin and cyclodextrin with appropriate antimicrobial and skin reconstruction properties are suitable alternatives that can accelerate wound healing and remove microbial infections. For instance, to improve the release profile of antibacterial agents such as metal nanoparticles and antibiotics, water-soluble polymers like polyethylene oxide and polyvinylpyrrolidone may be incorporated into polymeric nanofiber scaffolds. This review, therefore, addresses the current status and future challenges of antibacterial activities of nanofiber scaffolds composed of some of the natural occurring polymers.
Three-dimensional printing, also known as additive manufacturing, is a fabrication process whereby a 3D object is created layer-by-layer by depositing a feedstock material such as thermoplastic ...polymer. The 3D printing technology has been widely used for rapid prototyping and its interest as a fabrication method has grown significantly across many disciplines. The most common 3D printing technology is called the Fused Deposition Modelling (FDM) which utilises thermoplastic filaments as a starting material, then extrudes the material in sequential layers above its melting temperature to create a 3D object. These filaments can be fabricated using the Hot-Melt Extrusion (HME) technology. The advantage of using HME to manufacture polymer filaments for FDM printing is that a homogenous solid dispersion of two or more pharmaceutical excipients i.e., polymers can be made and a thermostable drug can even be introduced in the filament composition, which is otherwise impractical with any other techniques. By introducing HME techniques for 3D printing filament development can improve the bioavailability and solubility of drugs as well as sustain the drug release for a prolonged period of time. The latter is of particular interest when medical implants are considered via 3D printing. In recent years, there has been increasing interest in implementing a continuous manufacturing method on pharmaceutical products development and manufacture, in order to ensure high quality and efficacy with less batch-to-batch variations of the pharmaceutical products. The HME and FDM technology can be combined into one integrated continuous processing platform. This article reviews the working principle of Hot Melt Extrusion and Fused Deposition Modelling, and how these two technologies can be combined for the use of advanced pharmaceutical applications.
The purpose of this work was to evaluate the physicochemical and inhalation characteristics of different size fractions of a promising carrier, i.e., freeze-dried mannitol (FDM).
FDM was prepared and ...sieved into four size fractions. FDMs were then characterized in terms of micromeritic, solid-state and bulk properties. Dry powder inhaler (DPI) formulations were prepared using salbutamol sulphate (SS) and then evaluated in terms of drug content homogeneity and in vitro aerosolization performance.
The results showed that the crystalline state of mannitol was maintained following freeze-drying for all size fractions of FDM. All FDM particles showed elongated morphology and contained mixtures of α-, β- and δ-mannitol. In comparison to small FDM particles, FDMs with larger particle sizes demonstrated narrower size distributions, higher bulk and tap densities, lower porosities and better flowability.
Regardless of particle size, all FDMs generated a significantly higher (2.2–2.9-fold increase) fine particle fraction (FPF, 37.5±0.9%–48.6±2.8%) of SS in comparison to commercial mannitol. The FPFs of SS were related to the shape descriptors of FDM particles; however, FPFs did not prove quantitative apparent relationships with either particle size or powder bulk descriptors. Large FDM particles were more favourable than smaller particles because they produced DPI formulations with better flowability, better drug content homogeneity, lower amounts of the drug depositing on the throat and contained lower fine-particle-mannitol.
Optimized stable DPI formulations with superior physicochemical and pharmaceutical properties can be achieved using larger particles of freeze-dried mannitol (FDM).
Abstract
The therapeutic effectiveness of a chitosan encapsulated bacteriophage cocktail as a smart biocontrol agent was evaluated in this study to be used as a preventative and treatment option for ...gastrointestinal infections. To evaluate the effect of the bacteriophage formulation on the treatment of gastrointestinal infection, rats were infected with
Salmonella enterica
,
Shigella flexneri
, and
Escherichia coli
. The rats were weighed and their stools cultured. The results showed that the group which had the chitosan encapsulated bacteriophage cocktail did not lose weight after 3 days and had significantly lower group weight changes. Weight loss was significant in the rats that had cefixime administered instead. Positive cultured stools were reduced after 4 days compared to 2 days in the treated group with the chitosan encapsulated bacteriophage cocktail. The chitosan encapsulated bacteriophage cocktail can therefore be effective in the treatment of gastrointestinal infections.
•All recognized antibacterial and wound remedy mechanisms of ZnONPs are presented.•Comparison of antibacterial and wound healing capacities of chitosan, cellulose, alginate.•Micro/nano formulations ...of ZnONPs with chitosan, cellulose, and alginate.•Challenges and future viewpoints of ZnO nanoparticles with polysaccharides.
Release of Zn2+ ions from zinc oxide nanoparticles (ZnO NPs) is a major mechanism for oligodynamic activities of these metal oxide NPs against eukaryotic and prokaryotic microorganisms. In addition to this mechanism, ZnO NPs can form reactive oxygen species (ROSs) resulted from electron-hole formation under certain light wavelength. These properties with suitable biocompatibility and biodegradability of ZnO NPs compared to other metal NPs have caused higher applications of these nanomaterials in therapeutic and cosmetic fields. Recently, natural polymers including cellulose, chitosan, and alginate polymers have gained more attention as safe and cost-effective scaffold for wound healing. Both ZnO NPs and these polymers have not been able to satisfy related patients. In this way, the coupling of these materials and nanomaterials as nanocomposites (NCs) is an alternative way to increase the mechanical and antibacterial properties of wound-healing tissue scaffolds. Controllable release of Zn2+ ions in physiological medium should be considered as an indispensable factor to obtain appropriate industrial formulation. Therefore, in this review, attempts were made to highlight particularly important antibacterial results of these NCs in recent investigations.
Orally disintegrating tablets (ODTs) rapidly disintegrate or dissolve in the oral cavity without using water. Demand for ODTs has increased, and the field has overgrown in the pharmaceutical industry ...and academia. It is reported that ODTs have several advantages over other conventional tablets. Since some of them are absorbed from the mouth, pharynx, and esophagus as the saliva passes down into the stomach, in such cases, the bioavailability of the drug improves meaningfully. Furthermore, the immediate release property of ODTs makes them a popular oral dosage form in patients with swallowing challenges, children, and for cases with a need for rapid onset of action. The current review article explains the features of active ingredients and excipients used in the formulation of ODTs, discusses multiple ODT formulation and preparation techniques with their merits and demerits, and also, offers remedies for problems associated with ODTs. Moreover, quality control steps and required considerations are presented.
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•Curcumin with an anticancer effect showed a poor dissolution.•Crystallization of curcumin in absence of PVP led to formation of a new polymorph.•PVP in crystallization medium led to ...a remarkable dissolution enhancement.•The presence of PVP converted crystalline curcumin to amorphous curcumin.
Curcumin with a vast number of pharmacological activities is a poorly water soluble drug which its oral bioavailability is profoundly limited by its dissolution or solubility in GI tract. Curcumin could be a good anticancer drug if its solubility could be increased. Therefore, the aim of the present study was to increase the dissolution rate of curcumin by employing antisolvent crystallization technique and to investigate the effect of polyvinyl pyrrolidone K30 (PVP) as colloidal particles in crystallization medium on resultant particles. Curcumin was crystalized in the presence of different amounts of PVP by antisolvent crystallization method and their physical mixtures were prepared for comparison purposes. The samples were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and Fourier transform infrared spectroscopy (FT-IR). The solubility and dissolution of the treated and untreated curcumin were also determined. Antisolvent crystallization of curcumin led to the formation of particles with no definite geometric shape. It was interesting to note that the DSC and XRPD studies indicated the formation of a new polymorph and less crystallinity for particles crystallized in the absence of PVP. However, the crystallized curcumin in the presence of PVP was completely amorphous. All crystalized curcumin samples showed much higher dissolution rate compared to untreated curcumin. The amount of curcumin dissolved within 10 for treated curcumin in the presence of PVP (1:1 curcumin:PVP) was 7 times higher than untreated curcumin and this enhancement in the dissolution for curcumin samples crystallized in the absence of PVP was around 5 times. Overall‚ the results of this study showed that antisolvent crystallization method in the absence or presence of small amounts of PVP is very efficient in increasing the dissolution rate of curcumin to achieve better efficiency for curcumin.
In vitro dissolution and permeability testing aid the simulation of the in vivo behavior of inhalation drug products. Although the regulatory bodies have specific guidelines for the dissolution of ...orally administered dosage forms (e.g., tablets and capsules), this is not the case for orally inhaled formulations, as there is no commonly accepted test for assessing their dissolution pattern. Up until a few years ago, there was no consensus that assessing the dissolution of orally inhaled drugs is a key factor in the assessment of orally inhaled products. With the advancement of research in the field of dissolution methods for orally inhaled products and a focus on systemic delivery of new, poorly water-soluble drugs at higher therapeutic doses, an evaluation of dissolution kinetics is proving crucial. Dissolution and permeability testing can determine the differences between the developed formulations and the innovator's formulations and serve as a useful tool in correlating in vitro and in vivo studies. The current review highlights recent advances in the dissolution and permeability testing of inhalation products and their limitations, including recent cell-based technology. Although a few new dissolution and permeability testing methods have been established that have varying degrees of complexity, none have emerged as the standard method of choice. The review discusses the challenges of establishing methods that can closely simulate the in vivo absorption of drugs. It provides practical insights into method development for various dissolution testing scenarios and challenges with dose collection and particle deposition from inhalation devices for dissolution tests. Furthermore, dissolution kinetic models and statistical tests to compare the dissolution profiles of test and reference products are discussed.
This interdisciplinary review focuses on how flexible three-dimensional printing (3DP) technology can aid patients with neurological diseases. It covers a wide variety of current and possible ...applications ranging from neurosurgery to customizable polypill along with a brief description of the various 3DP techniques. The article goes into detail about how 3DP technology can aid delicate neurosurgical planning and its consequent outcome for patients. It also covers areas such as how the 3DP model can be utilized in patient counseling along with designing specific implants involved in cranioplasty and customization of a specialized instrument such as 3DP optogenetic probes. Furthermore, the review includes how a 3DP nasal cast can contribute to the development of nose-to-brain drug delivery along with looking into how bioprinting could be used for regenerating nerves and how 3D-printed drugs could offer practical benefits to patients suffering from neurological diseases via polypill.