Pharmaceutical Development and Technology

PURPOSE: Asses the wound healing activity of Polyvinyl alcohol - Deflazacort (PVA-DEF) nanofibers mats synthesized by electrospinning technology. METHODS: PVA-DEF nanofiber mats were created with various PVA polymer concentrations using an electrospinning process. The morphological features and diameter of the electrospun nanofibrous mats were investigated using scanning electron microscopy (SEM). The in vitro DEF release rate from PVA electrospun nanofibrous mats was evaluated...

The present study aimed to develop solid lipid nanoparticles of lutein (SLN/LT) with improved dissolution behavior and oral absorption. SLN/LT were prepared by a flash nanoprecipitation method using a multi-inlet vortex mixer, and their physicochemical, photochemical, and pharmacokinetic properties were evaluated. The mean particle size of SLN/LT re-dispersed in water was 237 nm, and small spherical particles with no significant aggregation were observed. LT significantly generated singlet oxygen upon exposure to pseudo-sunlight (250 W/m2 , 1 hour), suggesting its high photoreactivity...

In situ forming depots (ISFDs) represent attractive alternatives to the conventional sustained drug delivery systems. Carvedilol, a short half-life drug used on daily basis to manage chronic conditions, could benefit from this technology. The aim of this work was to develop, for the first time, a new injectable long-acting carvedilol-ISFD. Accordingly, 4 different grades of polyesters with varying properties as i) lactide to glycolide ratio (polylactide-co-glycolide (PLGA) vs. polylactide (PLA)), and ii) end functionality (acid- vs...

The necessity for personalized patient treatment has drastically increased since the contribution of genes to the differences in physiological and metabolic state of individuals have been exposed. Different approaches have been considered so far in order to satisfy all of the diversities in patient needs, yet none of them have been fully implemented thus far. In this framework, various types of 2D printing technologies have been identified to offer some potential solutions for personalized medication, which development is increasing rapidly...

The aim was to investigate eutectic transition during tableting and storage. Mixtures of lidocaine and series of NSAIDs with increasing melting point were used as model systems to guide formulators to scaleup eutectic forming materials gaining enhanced dissolution while avoiding deleterious physical changes. Physical mixtures of NSAIDs with lidocaine were prepared at eutectic forming ratio. These were directly compressed, dry co-ground before compression or compressed after wet granulation. Dissolution of tablets were compared to corresponding dry co-ground mixture...

Poly (D, L Lactic-co-Glycolic acid) (PLGA) is an FDA-approved polymer. It is distinguished from other biocompatible polymers by its feasibility of production and safety for intravenous cancer tumor targeting. Curcumin (CUR) is a natural molecule with versatile bioactivities including inhibiting the nuclear Factor kappa B (Nf-kB) levels in cancer cells, increased by chemotherapy agents. Our group previously reported a successful decrease in the p65 (RelA) subunit of Nf-kB using 125μg/ml CUR loaded into PLGA nano-micelles...

The study developed and evaluated Sorafenib Tosylate (SRT)-loaded polymeric microparticles (MPs) using biodegradable polymer polycaprolactone (PCL) as a potential inhalable carrier for NSCLC. MPs were prepared by spray-drying an oil-in-water (o/w) emulsion. The optimized MPs demonstrated excellent flowability, particle size of 2.84 ± 0.5 μm, zeta potential of -14.0 ± 1.5 mV, and 85.08 ± 5.43% entrapment efficiency. ATR-FTIR/DSC studies revealed a lack of characteristic peaks of the crystalline drug signifying good entrapment of the drug...

Fungal skin diseases are recognized as a global burden disease that affect human quality adjusted life. Terbinafine belongs to allylamine and broad-spectrum antifungal drugs but considered practically insoluble. Different lipids/surfactant with two different molar ratios were investigated with Span 40-based niosomes; characterized for size, morphology, loading capacity (EE%), in vitro release, kinetics and antifungal activities. Vesicle sizes (0.19 to 1.23 µm), EE% (25% to 99%), zeta potential (> -32 mV) and in vitro release rates were dependent on both lipid types and ratios...

Evolving therapeutic landscape through combinatorial chemistry and high throughput screening have resulted in an increased number of poorly soluble drugs. Drug delivery strategies quickly adapted to convert these drugs into successful therapies. Amorphous solid dispersion (ASD) technology is widely employed as a drug delivery strategy by pharmaceutical industries to overcome the challenges associated with these poorly soluble drugs. The development of ASD formulation requires an understanding of polymers and manufacturing techniques...

The efficacy and safety of chemotherapy are two major challenges when it comes to treating ovarian cancer. The associated undesirable side effects of chemotherapy agents jeopardize the clinical intent and the efficiency of the therapy. Multiple studies have been published describing new developments and novel strategies utilizing the latest therapeutic and drug delivery technologies to address the efficacy and safety of chemotherapeutics in ovarian cancers. We have identified five novel technologies that are available and, if used, have the potential to mitigate the above-mentioned challenges...

Skin disorders are preferentially treated by topical administration of medicines or cosmetics because of the possibility of local action. However, a great concern is the delivery of topical actives with effective penetration through the stratum corneum to ensure the desired effect. Considering the search for a carrier system that allows the penetration/permeation of active pharmaceutical ingredients through this structure, searching for effective topical pharmaceutical forms is needed. Foams have been widely studied over the years due to their high capacity to favor the active to overcome the cutaneous barrier and because this form of presentation has ease of application and high acceptability by users...

Rheumatoid arthritis (RA) is a chronic autoimmune disease which affects around 1% globally leading to joint inflammation and disability. Etorocoxib (ETR) is a potent COX-2 inhibitor traditionally used orally to alleviate RA induced inflammation, yet it causes hepatic side effects on prolonged use. This study aims for in silico optimization of ETR polyelectrolyte complex (PEC) utilizing Chondroitin sulphate (CS) and Chitosan (CH) for transdermal delivery to RA-inflamed joints with a synergistic anti-inflammatory action owing to CS...

Exploitation of advanced methotrexate (MTX) delivery with nanocomposites has important clinical application value. Poloxamer 188 micelle and layered double hydroxide loaded with MTX (LDH-MTX) by exfoliation reassembling were used to prepare LDH-MTX-poloxamer 188 nanocomposites with good dispersibility and efficient cellular uptake for controlled drug delivery. The LDH-MTX-poloxamer 188 nanocomposites with sphere-like morphology, of which the average hydrodynamic diameter was <100 nm, were shown to have better dispersion state than naked LDH-MTX...

In the present study, novel gastroretentive bilayer tablets were developed that are promising for the once-a-day oral delivery of the drug candidate MT-1207. The gastroretentive layer consisted of a combination of hydrophilic and hydrophobic polymers, namely polyethylene oxide and Kollidon® SR. A factorial experiment was conducted, and the results revealed a non-effervescent gastroretentive layer that, unlike most gastroretentive layers reported in the literature, was easy to prepare, and provided immediate tablet buoyancy (mean floating lag time of 1...

A graphical plot of drug stability-study data can be extrapolated to estimate the drug's percent degradation and therefore its shelf-life beyond the time period of the study. However, after a statistical confidence limit is applied, that shelf-life estimate is significantly reduced. Such a reduction can be minimized by transforming the data so that it plots as close as possible to linearity, a process that is called reliability plotting. Reliability plotting seems to have been rarely if ever used on drug stability data, despite its being mentioned in relevant guidance documents and its ability to justify longer shelf-life at no additional cost...

Low value of deformation before crushing is an obvious and understandable measure for brittleness of materials including tablets. In this paper three methods based on deformation measurement in a flexure tester is compared. The simplest one is a plain measurement of distance from contact or selected start point till fracture. Next the brittle-ductile method (BDI), where the distance is established by normalisation of the force-displacement curve based on the work of failure (WOF). The third method is the tablet brittleness index (TBI) by Gong and Sun, where the reciprocal of a linear distance is proposed as a brittleness quantity...

Dermal drug delivery has emerged as a promising alternative to traditional methods of drug administration due to its non-invasive nature and ease of use. However, the stratum corneum, the outermost layer of the skin, presents a significant barrier to drug penetration. Niosomes, self-assembled vesicular structures composed of nonionic surfactants and cholesterol, have been extensively investigated as a means of overcoming this barrier and improving the efficacy of dermal drug delivery. This review summarizes the current state of research on the use of niosomes in dermal drug delivery in cosmetics, with a particular focus on their formulation, characterization, and application in the delivery of various drug classes...

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%)...