Pharmaceutical Development and Technology

The objective of this study was to improve the solubility and inhibit the crystallisation during the gastric-to-intestinal transfer of Erlotinib (ERL), a small molecule kinase inhibitor (smKI) compound class, which is classified as class II drug in the Biopharmaceutical Classification System (BCS). A screening approach combining different parameters (solubility in aqueous media, inhibitory effect of drug crystallisation from supersaturated drug solutions) was applied to selected polymers for the development of solid amorphous dispersions of ERL...

Abstract-Milling affects not only particle size distributions but also other important granule quality attributes, such as API content and porosity, which can have a significant impact on the quality of the final drug form. The ability to understand and predict the effects of milling conditions on these attributes is crucial. A hybrid population balance model (PBM) was developed to model the Comil, which was validated using experimental results with an R 2 of above 0.9. This presented model is dependent on the process conditions, material properties and equipment geometry, such as the classification screen size...

Vomiting is a common symptom associated with migraine. Metoclopramide (MCP) is used as an effective treatment for managing the pain of migraine attack and vomiting. Buccal films loaded with MCP formulated using the solvent casting method. The films were transparent, homogenous, and easily removed after drying. The weight and thickness of the films increased with increasing the drug content as cm2 of the film. All films' endurance indicated flexibility of the prepared films. Drug content investigation showed higher MCP entrapment (>90%)...

Lamotrigine (LTG) is a second-generation antiepileptic drug that belongs to Biopharmaceutics Classification System (BCS) class II. LTG has a low probability of crossing the BBB if administered orally. This study was designed to fabricate LTG cubosomal dispersion that is further loaded in a thermosensitive in situ gel to increase nasal residence time and enhance drug absorption across the nasal mucosal membrane. LTG-loaded cubosomes exhibited an entrapment efficiency ranging from 24.83% to 60.13%, a particle size ranging from 116...

Rivaroxaban (RXB), a novel Xa inhibitor having groundbreaking therapeutic potential. However, this drug is associated with few limitations, including its pharmacokinetics related toxicities. Here, we developed RXB-loaded SLNs (RXB-SLNs) to improve its biopharmaceutical profile. High pressure homogenizer was used to prepare RXB-SLNs, followed by their particle characterization, Transmission electron microscopy (TEM), Dynamic light scattering (DSC) and Powder X-ray diffraction (PXRD) analysis. Beside this, in-vitro, ex-vivo and in-vivo evaluation, prothrombin time assessment and toxicity was investigated...

The objective of this study was to develop novel invaethosomes (I-ETS) and invaflexosomes (I-FXS) to enhance the dermal delivery of clotrimazole (CZ). Twenty model CZ-loaded I-ETS and I-FXS formulations were created according to a face-centered central composite experimental design. CZ-loaded vesicle formulations containing a constant concentration of 0.025% w/v CZ and various amounts of ethanol, d-limonene and polysorbate 20 as penetration enhancers were prepared using the thin film hydration method. The physicochemical characteristics, skin permeability and antifungal activity were characterized...

Non-alcoholic fatty liver disease is one of the leading causes of death worldwide. Even if with such a high mortality there is no definite treatment approved. Thus, there is a need to develop a formulation which can have multiple pharmacological activities. Herbal drugs are among the most promising compounds that act by different pharmacological actions. For increasing the bio-activity of Silymarin we had isolated five active biomarker molecules from silymarin extract (as a Phytopharmaceutical) in our previous work...

PURPOSE: This work aimed to fabricate alginate based in-situ gelling matrix of vildagliptin improved by calcium and carboxy methyl cellulose (CMC) for appropriate adjustment of the onset and duration of action. This easy-to-swallow thickened liquid preparation aimed to improve compliance for dysphagic or elderly diabetic patients. METHODS: Vildagliptin dispersions containing alginate were fabricated in the presence or absence of calcium chloride to assess the effect of calcium ion, then a matrix containing 1...

This study aimed to evaluate a material sparing method to predict tabletability and compactibility relationships. Seven α -lactose monohydrate powders with varying particle size were used as test materials. The compressibility of the powders was determined experimentally, whereas tabletability and compactibility profiles were derived both experimentally and predicted. In the prediction method, two experimental compression parameters (Kawakita <mml:math xmlns:mml="https://www.w3.org/1998/Math/MathML"><mml:mrow><mml:msup><mml:mrow><mml:mi>b</mml:mi></mml:mrow><mml:mrow><mml:mo>-</mml:mo><mml:mn>1</mml:mn></mml:mrow></mml:msup></mml:mrow></mml:math> and Heckel plastic stiffness) and a single tensile strength reference value were used, all necessary data obtained from a single compression experiment...

The aim was to enhance the dissolution rate and in vivo efficacy of flubendazole against trichinella spiralis. Flubendazole nanocrystals were developed by controlled anti-solvent recrystallization. Saturated flubendazole solution was prepared in DMSO. This was injected into phosphate buffer (pH 7.4) containing Aerosil 200, Poloxamer 407 or sodium lauryl sulphate (SLS) while mixing using paddle mixer. The developed crystals were separated from DMSO/aqueous system by centrifugation. The crystals were characterized using DSC, X-ray diffraction and electron microscopy...

Exosomes are one type of extracellular vesicles with size ranging from 30 to 150 nm, which are involved in intercellular communication by transporting specific proteins, nucleic acids, and low molecular weight metabolites. The size and competence of exosomes to transfer biological materials to recipient cells have made them suitable for biomedical use. Therefore, exosomes have been studied as drug delivery systems for various diseases due to low immunogenicity, preferred tumor homing, innate and acquired targetability, and stability...

The aim of the study was to enhance curcumin skin permeability through the preparation of spanlastics. Spanlastics were prepared using the ethanol injection technique through a central composite design using Span 60 concentration (X1 ), edge activator type (X2 ), and its concentration (X3 ) as the independent variables. The spanlastics were characterized for particle size (PS), encapsulation efficiency (EE), and dissolution efficiency (%DE24h ). Formulae with the highest desirability (FN1 and FN2) were prepared and further characterized...

The aim of this study is to prepare and characterise mucoadhesive silica-coated silver nanoparticles loaded with ciprofloxacin (S-AgNPs-CSCFX), and investigate serum biochemical, haematological, and histopathological effects in Sprague Dawley rats upon oral administration. S-AgNPs-CSCFX microparticles were prepared using three fluid nozzle spray drying and characterised by scanning electron microscopy (SEM), X-ray dispersive spectrometry (EDX), transmission electron microscopy (TEM), Fourier transform infrared (FTIR), zeta potential and particles size measurements and X-ray powder diffraction (XRPD)...

The environmental can modify the physiology and body protective function of skin. Propolis (PRP) and curcumin (CUR) possess important antioxidant and antimicrobial properties, and they can be administered in the combined way and using photodynamic therapy (PDT). Emulgels can control the drug release due to the physicochemical properties of the gel and the emulsion. They constitute a good strategy for achieving an improved platform for combined delivery of PRP and CUR. There are no other studies of emulgels composed of PRP and CUR and their performance as antimicrobial and skin healing using or not PDT...

In this work, novel carriers- nanoemulsomes (NE) of Ganciclovir (GCV) and a fluorescent marker sodium fluorescein (SF) were developed and evaluated for posterior ocular delivery via topical route. GCV loaded emulsomes (GCV NE) were optimized by a factorial design and various characterization parameters were performed on the optimized batch. The optimized batch had particle size of 131.04 ± 1.87 nm, % entrapment efficiency of 36.42 ± 3.09% and its TEM image showed discrete spherical structures below 200nm...

Immunotherapy is a promising cancer treatment strategy. In contrast, PD-1/PD-L1 inhibitors are associated with low response rates and are only useful in a small group of cancer patients. A combination of treatments may be effective for overcoming this clinical issue. Preladenant is an adenosine receptor inhibitor that can block the adenosine pathway and improve the tumor microenvironment (TME), thereby enhancing the immunotherapeutic effect of PD-1 inhibitors. However, its poor water solubility and low targeting limit its clinical applications...

Temperature-sensitive drug delivery systems (TSDDS) are one of the systems that have received more attention in medical science these days due to their advantages. As these systems are sensitive to temperature, drug delivery to the target becomes more specific. Temperature-sensitive nanogels have many applications, including microbial infections, cancer therapy, transdermal use and tissue repair. These systems are characterized by minimal toxicity, improved therapeutic efficacy and reduced exposure to normal cells...

This study aimed to improve the use of YF8, a matrine derivative obtained through chemical transformation of matrine extracted from Sophora alopecuroides . YF8 has demonstrated improved cytotoxicity compared to matrine, but its hydrophobic nature hinders its application. To overcome this, the lipid prodrug YF8-OA was synthesized by linking oleic acid (OA) to YF8 through an ester bond. Although YF8-OA could self-assemble into unique nanostructures in water, it was not sufficiently stable. To enhance the stability of YF8-OA lipid prodrug nanoparticles (LPs), we employed the strategy of PEGylation using DSPE-mPEG2000 or DSPE-mPEG2000 conjugated with folic acid (FA)...

To enhance the oral bioavailability of atorvastatin calcium (ATV), a novel solidified micelle (S-micelle) was developed. Two surfactants, Gelucire 48/16 (G48) and Tween 20 (T20), were employed for micelle formation, and two solid carriers (SC), Florite PS-10 (FLO) and Vivapur 105 (VP105), were selected as solid carriers. The S-micelle was optimized using a Box-Behnken design with three independent variables, including G48:T20 (X1 , 1.8:1), SC:G48 + T20 (X2 , 0.65:1), and FLO:VP105 (X3 , 1.4:0...

Lung cancer ranks second position among the cancer-related deaths. Osimertinib mesylate (OSM) is a tyrosine-kinase-inhibitor which can effectively treat NSCLC, but still there are certain limitations and side effects which could be circumvented by polymeric nanoparticles approach. Hence, this research was aimed to develop drug-loaded biodegradable poly caprolactone nanoparticles (PCL-NPs) such as OSM-loaded PCL-NPs (PCL-OSM-NPs) and chitosan fabricated OSM-loaded PCL-NPs (CS-PCL-OSM-NPs) to achieve active-targeting of OSM in the cancerous lung tissue...