Fabrication of extended-dissolution divalproex tablets: a green solvent-free granulation technique.

Divalproex sodium (DVS) is a challenging drug owing to its hygroscopicity, bitter taste, and short half-life. This study aims to produce stable taste masked DVS once daily tablets using solvent free hot melt granulation (HMG) process. A lab scale high shear mixer granulator employing six meltable lipid binders (compritol888 ATO, beeswax, gelucire50/13, precirol ATO5, stearyl alcohol, and geleol) was used for the preparation of tablets.

Optimisation of the microencapsulation of lavender oil by spray drying.

Lavender oil consists of around 100 components and is susceptible to volatilisation and degradation reactions. Microencapsulate lavender oil by spray drying using a biocompatible polymeric blend of gum acacia and maltodextrin to protect the oil components. Effect of total polymer content, oil loading, gum acacia, and maltodextrin proportions on the size, yield, loading, and encapsulation efficiency of the microparticles was investigated.

Enhancing the Intestinal Permeation of the Chondroprotective Nutraceuticals Glucosamine Sulphate and Chondroitin Sulphate Using Conventional and Modified Liposomes.

Background: Liposomes are promising systems for the delivery of macromolecules and poorly absorbed drugs, owing to their ability to compartmentalize drugs, their biodegradability and biocompatibility.

Objective: The aim of the present study was to formulate and evaluate conventional and modified glucosamine sulphate (GluS) and chondroitin sulphate (CS) liposomal formulations, to enhance their oral permeation for the treatment of osteoarthritis (OA).

Method: Liposomal formulations were prepared by the thin-film hydration method using two types of phospholipids; Epikuron 200© and Epikuron 200© SH, and three permeation enhancers; poloxamer 407, cetylpyridinium chloride, and sodium deoxycholate.

Geriatric-Oriented High Dose Nutraceutical ODTs: Formulation and Physicomechanical Characterization.

Context: Oral disintegrating tablets (ODTs) represent a better option than conventional tablets for geriatric population, owing to their fast onset of action and their better patient compliance.

Objective: Two principal therapeutic high-dose nutraceuticals; chondroitin sulphate and glucosamine were formulated into an oral disintegration tablet (ODT) intended for sublingual administration, and optimized to improve compliance and achieve rapid onset of action in osteoarthritis treatment.

Materials And Methods: Different formulations were prepared either by melt granulation or direct compression techniques.

Jojoba Oil Soft Colloidal Nanocarrier of a Synthetic Retinoid: Preparation, Characterization and Clinical Efficacy in Psoriatic Patients.

Background: Nanotechnology has provided substantial benefits in drug delivery, especially in the treatment of dermatological diseases. Psoriasis is a chronic inflammatory skin disease in which topical delivery of antipsoriatic agents is considered the first line treatment.

Objective: To investigate whether the encapsulation of the synthetic retinoid tazarotene in a nanocarrier based on jojoba oil would decrease its irritation potential and clinically improve its therapeutic outcome in psoriatic patients.

Optimizing the dermal accumulation of a tazarotene microemulsion using skin deposition modeling.

Context: It is well known that microemulsions are mainly utilized for their transdermal rather than their dermal drug delivery potential due to their low viscosity, and the presence of penetration enhancing surfactants and co-surfactants.

Objective: Applying quality by design (QbD) principles, a tazarotene microemulsion formulation for local skin delivery was optimized by creating a control space.

Materials And Methods: Critical formulation factors (CFF) were oil, surfactant/co-surfactant (SAA/CoS), and water percentages.

A highlight on lipid based nanocarriers for transcutaneous immunization.

Transcutaneous vaccination has become a widely used technique for providing immunity against several types of pathogens, taking advantage of the immune components found in the skin. The success in the field of vaccination has not only relied on the type of antigen and adjuvant delivered, but also on how they are delivered. In this regard, particulate carriers, especially nanoparticles have evoked considerable interest, owing to the desirable properties that they impart to the substance being delivered.

Lipid based nanocapsules: a multitude of biomedical applications.

Lipid nanocapsules with their unique composition represent a promising biocompatible drug delivery platform in nanometer range with narrow size distribution. They are highly stable in comparison to other nano-vectors and were found to impart very desirable characteristics to the therapeutic molecule being delivered within. The current review sheds the light on the methods of preparation of lipid nanocapsules, which are simple and easily scalable, in addition to providing examples of post insertion of some compounds for prolonging vascular circulation, protection, and targeting several diseases.

Study of radial die-wall pressure during high speed tableting: effect of formulation variables.

With high-speed compaction cycles as applied in pharmaceutical industrial presses, robust tools like radial die-wall pressure (RDWP) are required to monitor the deformation behavior of formulations under pressure and to avoid common problems such as capping. In this study, the effects of common formulation factors such as lubricant, binder, and drug loading on RDW were investigated. Compaction simulation using Presster™ was applied for five pharmaceutical fillers with different compaction behaviors.

Investigating the effect of punch geometry on high speed tableting through radial die-wall pressure monitoring.

Dwell time mainly depends on punch geometry, so some tableting problems such as capping and lamination could occur at high speed compaction. Robust tools are required to monitor the interaction of punch tip and powder bed at these high speeds. Our aim was to investigate the effect of punch geometry (flat and standard concave) on powder compaction at high speed using radial die-wall pressure (RDWP) as a monitoring tool.

A novel tool for the prediction of tablet sticking during high speed compaction.

During tableting, capping is a problem of cohesion while sticking is a problem of adhesion. Sticking is a multi-composite problem; causes are either material or machine related. Nowadays, detecting such a problem is a pre-requisite in the early stages of development.

Investigating the effect of particle size and shape on high speed tableting through radial die-wall pressure monitoring.

Investigating particle properties such as shape and size is important in understanding the deformation behavior of powder under compression during tableting. Particle shape and size control the pattern of powder rearrangement and interaction in the die and so the final properties of the compact. The aim of this study was to examine the effect of particle size and shape on compactability.

Radial die-wall pressure as a reliable tool for studying the effect of powder water activity on high speed tableting.

The effect of moisture as a function of water activity (Aw) on the compaction process is important to understand particle/water interaction and deformation. Studying powder/moisture interaction under pressure with radial die-wall pressure (RDWP) tool was never done. The aim of our study was to use this tool to study this interaction at high compression pressure and speed.

Study of radial die-wall pressure changes during pharmaceutical powder compaction.

Context: In tablet manufacturing, less attention is paid to the measurement of die-wall pressure than to force-displacement diagrams.

Objective: Therefore, the aim of this study was to investigate radial stress change during pharmaceutical compaction.

Materials And Methods: The Presster(TM), a tablet-press replicator, was used to characterize compaction behavior of microcrystalline cellulose (viscoelastic), calcium hydrogen phosphate dihydrate (brittle), direct compressible mannitol (plastic), pre-gelatinized starch (plastic/elastic), and spray dried lactose monohydrate (plastic/brittle) by measuring radial die-wall pressure; therefore powders were compacted at different (pre) compaction pressures as well as different speeds.

A novel formulation for mebeverine hydrochloride.

The antispasmodic drug mebeverine hydrochloride was formulated into a film-forming gel to be used as a topical local anesthetic. A mixture of cellulose derivatives was used as a base. Additives were used to enhance the release as well as the residence time.

Formulation of an antispasmodic drug as a topical local anesthetic.

Mebeverine hydrochloride, a spasmolytic agent on GIT smooth muscles, was reported to have a local anesthetic effect. Thus, it was desired in this study to formulate mebeverine HCl into a gel that could be used locally in the treatment of different oral painful conditions. Poloxamer 407 (P-407) was used as the base for this gel.