Drug Development and Industrial Pharmacy

UNLABELLED: Objective TheDES are formed by mixing a Hydrogen Bond Donor (HBD) and a Hydrogen Bond Acceptor (HBA) in appropriate molar ratios. These solvents have been shown to enhance drug solubility, permeability, and delivery. The main objective of the present article is to review these advantages of TheDES. SIGNIFICANCE: TheDES show unique properties, such as low toxicity, biodegradability, improved bioavailability and enhanced drug delivery of poorly soluble active pharmaceutical ingredients...

Objective: Belonging to the class II drugs according to the biopharmaceutics classification system, silibinin (SLB) benefits from high permeability but suffers poor solubility that negatively affects the development of any delivery system. This research aimed to improve SLB solubility by combined use of co-solvency and complexation phenomena. Methods: Solubility studies were performed using the phase solubility analysis according to the shake-flask method in the presence of ethanol and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) as a co-solvent and inclusion complexing agent, respectively...

OBJECTIVE: The aim of the present study was to develop and optimize a wound dressing film loaded with chloramphenicol (CAM) and ibuprofen (IBU) using a Quality by Design (QbD) approach. SIGNIFICANCE: The two drugs have been combined in the same dressing as they address two critical aspects of the wound healing process, namely prevention of bacterial infection and reduction of inflammation and pain related to injury. METHODS: Three critical formulation variables were identified, namely the ratios of Kollicoat SR 30D, polyethylene glycol 400 and polyvinyl alcohol...

OBJECTIVE: Ferulic acid (FA) is a promising nutraceutical molecule which exhibits antioxidant and anti-inflammatory properties, but it suffers from poor solubility and bioavailability. In the presented study, FA nanoemulsions were prepared to potentiate the therapeutic efficacy of FA in prevention of gastric ulcer. METHODS: FA nanoemulsions were prepared, pharmaceutically characterized, and the selected nanoemusion was tested for its ulcer-ameliorative properties in rats after induction of gastric ulcer using ethanol, by examination of stomach tissues, assessment of serum IL-1β and TNF-α, assessment of nitric oxide, prostaglandin E2, glutathione, catalase and thiobarbituric acid reactive substance in stomach homogenates, as well as histological and immunohistochemical evaluation...

OBJECTIVE: The study evaluated physicochemical properties of eight different polymeric nanoparticles (NPs) and their interaction with lung barrier and their suitability for pulmonary drug delivery. METHODS: Eight physiochemically different NPs were fabricated from Poly lactic-co-glycolic acid (PLGA, PL) and Poly glycerol adipate-co-ω-pentadecalactone (PGA-co-PDL, PG) via emulsification-solvent evaporation. Pulmonary barrier integrity was investigated in vitro using Calu-3 under air-liquid interface...

Objective: This research aimed to investigate the application of the coaxial electrospun method for the production of natural extracts (papaya leaf extract) fibre films. This was achieved through utilising different polymers and with a focus on the conductivity and the viscosity of polymer solutions as critical parameters to generate successful fibres. Significance: Electrospinning is a promising trending manufacturing method for incorporating thermolabile herbal extracts using coaxial electrospun features...

OBJECTIVE: The purpose of this research was to determine any connections between the characteristics of oleogels made of beeswax and the impact of mango butter. METHODS: Oleogel was prepared through inverted tube methods, and optimized through oil binding capacity. Other evaluations like bright field and polarized microscopy, fourier-transform infrared (FTIR) spectroscopy, crystallization kinetics, mechanical study, and X-ray diffractometry (XRD). The drug release kinetic studies and in vitro antibacterial studies were performed...

OBJECTIVE: The study was aimed at formulating Temozolomide (TMZ) loaded gelatin nanoparticles (GNPs) encapsulated into polyvinyl alcohol (PVA) nanofibers (TMZ-GNPs-PVA NFs) as the nano-in-nanofiber delivery system. The secondary objective was to explore the sustained releasing ability of this system and to assess its enhanced cellular uptake against U87MG glioma cells in vitro. SIGNIFICANCE: Nano - in - nanofibers are the emerging drug delivery systems for treating a wide range of diseases including cancers as they overcome the challenges experienced by nanoparticles and nanofibers alone...

Objectives: Development and evaluation of a novel human stratum corneum (SC) mimetic phospholipid vesicle-based permeation assay (PVPASC ) model for in vitro permeation studies. Significance: Due Owing to the increasing restrictions ion the use of human and animal skins, artificial skin models have attracted lots of substantial interest in pharmaceuticals and cosmetic industrials. In this study, a modified PVPASC model containing both SC lipids and proteins was developed. Methods: The PVPASC model was optimized by altering changing the lipid composition and adding keratin in the formulation of large liposomes...

The overactive bladder is a condition characterized by a sudden urge to urinate, even with small volumes of urine present in the bladder. The current treatments available for this pathology consist on conservative approaches and the continuous administration of drugs, which when made by conventional methods has limitations related to the first pass metabolism, bioavailability, severe side effects, and low patient adherence to treatments, ultimately leading to low effectiveness. Within this context, the present work proposes the design, manufacture, and characterization of an intravesical implant for the treatment of overactive bladder pathology, using EVA copolymer as a matrix and oxybutynin as a drug...

OBJECTIVE: The purpose of the present study was to formulate a menantine hydrochloride (MH) sustained-release suspension. METHODS: Menantine hydrochloride drug resin complex (MH-DRC) was prepared with strong acid cation exchange resin as carrier using water bath method. The MH-DRC was characterized using scanning electron microscopy, X-ray diffraction and infrared spectroscopy. The MH-coated microcapsule (MH-CM) with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension...

OBJECTIVE: Development of non-toxic and stable fluorescent emission B-Cu nanoclusters (NCs) for the specific detection of dopamine at low concentrations in cerebrospinal fluid (CSF). SIGNIFICANCE: Fluorescent gold and copper nanoclusters conjugated with proteins, such as Bovine Serum Albumin (BSA), offer photostability and healthcare potential. This study focused on fabricating B-Cu NCs that exhibited superior characteristics, for sensitive dopamine detection. METHODS: The study employed various instrumental techniques including Attenuated Total Reflectance Fourier-Transform Infrared Spectroscopy (ATR-FTIR), Scanning Electron Microscopy (SEM), Spectrofluorometry, and Transmission Electron Microscopy (TEM) to characterise the formulated B-Cu NCs...

UNLABELLED: Objective Magnolol (MG) and Brucea javanica (L.) Merr. oil (BJO) possess synergetic anti-tumor effects, but have poor water solubility and stability, which results in low oral bioavailability. SIGNIFICANCE: The MG loaded self-microemulsion drug delivery system (MG-SMDDS) with BJO as oil phase component was utilized to improve the cellular uptake and synergetic anti-tumor effects. METHODS: Compatibility study and pseudoternary phase diagram (PTPD) were respectively employed to screen for the composition and proportion of oil phase in the formulation...

Objectives: This study aimed to determine the incidence, types and predictors of Potentially Harmful Excipients (PHE) exposure among hospitalized neonates. Methods: A prospective observational study was conducted from March to April 2022 in neonatal wards at a state hospital in Malaysia. The PHEs of interest were aspartame, benzalkonium chloride, benzyl alcohol, benzoic acid or benzoates, ethanol, parabens, polysorbate 80, propylene glycol, saccharin sodium, sorbitol and sulphites. Product information leaflets (PILs) and summaries of product characteristics (SPCs) were referred to obtain information on active pharmaceutical ingredient, strength, trade name as well as type and amount of the excipients...

Objective: The purpose of this study was to formulate, optimise Ozenoxacin topical nano-emulsion using factorial design followed by to prepare and evaluate nano-emulgel using validated In-Vitro Release Testing (IVRT) technique for determination of Ozenoxacin release rate along with Ex-Vivo Permeation Testing (EVPT). Significance: Nano-emulgel are a proven delivery system for poorly soluble substances works by enhancing the solubility and bioavailability. Factorial design provides a systematic and efficient means to study the effect of multiple factors on responses...

OBJECTIVE: To develop a sensitive and fast detection method via ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) to assess the concentration of ajuforrestin A, ajuforrestin B, ajugamacrin and 8-O-Acetylharpagide primarily derived from Ajuga plants in mice blood and their pharmacokinetics. METHODS: Single protein precipitation with high-proportioned acetonitrile is chosen for sample clean-up. The UPLC HSS T3 (2.1 mm × 100 mm, 1...

Objective: This study aimed to optimize the formulation of carbidopa/levodopa orally disintegrating tablets (ODTs) in order to improve their disintegration performance, and facilitate easier medication intake for Parkinson's patients. Method: The response surface methodology (RSM) was used to optimize the formulation, with the content of cross-linked polyvinylpyrrolidone (PVPP), microcrystalline cellulose (MCC), and mannitol (MNT) as independent variables, and disintegration time as the response parameter. Python was utilized to model Carr Indices and mixing time to determine the suitable mixing time...

ObjectivesThis study aimed to develop, optimize and evaluate glyceryl monooleate (GMO) based cubosomes as a drug delivery system containing cisplatin for treatment of human lung carcinoma.SignificanceThe significance of this research was to successfully incorporate slightly water soluble and potent anticancer drug (cisplatin) into cubosomes, which provide slow and sustained release of drug for longer period of time.MethodsThe delivery system was developed through top-down approach by melting GMO and poloxamer 407 (P407) at 70 °C and then drop-wise addition of warm deionized water (70 °C) containing cisplatin...

Background: Triamterene is an oral antihypertensive drug with dissolution-limited poor bioavailability. It can be used as monotherapy or in fixed dose combination with hydrochlorothiazide which also suffers from poor dissolution. Moreover, co-processing of drugs in fixed dose combination can alter their properties. Accordingly, pre-formulation studies should investigate the effect of co-processing and optimize the dissolution of drugs before and after fixed dose combination. This is expected to avoid deleterious interaction (if any) and to hasten the biopharmaceutical properties...

OBJECTIVE: This study aimed to investigate the impact of physical solid dispersions of spray-dried glibenclamide (SG) on the surface of microcrystalline cellulose (MC) and mannitol (M) surfaces, as well as their combination with phosphatidylcholine (P), on enhancing the dissolution rate of glibenclamide (G). METHODS: Solid dispersions were prepared using varying proportions of 1:1, 1:4 and 1:10 for SG on the surface of MC (SGA) and M (SGM), and then combined with P, in a proportion of 1:4:0...