Hydroxypropyl methyl cellulose, HPMC, a hydrophilic polymer, is widely used for the development of extended release hydrophilic matrices and it is also considered as a good contender for the fabrication of 3D printing of matrix tablets. It is often combined with plasticisers to enable extrusion. The aim of the current project was to develop plasticizer-free 3D printed hydrophilic matrices using drug loaded filaments prepared via HME to achieve an in vitro (swelling, erosion and drug release) and in vivo (drug absorption) performance which is analogous to hydrophilic matrix tablets developed through conventional approaches. Additionally, the morphology of the printed tablets was studied using quantitative 3D surface texture studies and the porosity calculated. Filaments were produced successfully and used to produce matrix tablets with acceptable drug loading (95–105%), mechanical and surface texture properties regardless of the employed HPMC grade. The viscosity of HPMC had a discernible impact on the swelling, erosion, HPMC dissolution, drug release and pharmacokinetic findings. The highest viscosity grade (K100M) results in higher degree of swelling, decreased HPMC dissolution, low matrix erosion, decreased drug release and extended drug absorption profile. Overall, this study demonstrated that the drug loaded (glipizide) filaments and matrix tablets of medium to high viscosity grades of HPMC, without the aid of plasticisers, can be successfully prepared. Furthermore, the in vitro and in vivo studies have revealed the successful fabrication of extended release matrices.
Overactive bladder syndrome (OAB) is characterised by urgency symptoms, with or without urgency incontinence, usually with frequency and nocturia and severely affects the quality of life. This systematic review evaluates the various drug delivery strategies used in practice to manage OAB. Advanced drug delivery strategies alongside traditional strategies were comprehensively analysed and comparatively evaluated. The present review was conducted according to the preferred reporting items for systematic reviews and meta-analyses guidelines. A total of 24 studies reporting the development of novel formulations for the treatment of OAB were considered eligible and were further categorised according to the route of drug administration. The review found that various drug delivery routes (transdermal, intravesicular, oral, vaginal and intramuscular) are used for the administration of drugs for managing OAB, however, the outcomes illustrated the marked potential of transdermal drug delivery route. The findings of the current review are expected to be helpful for pharmaceutical scientists to better comprehend the existing literature and challenges and is anticipated to provide a basis for designing and fabricating novel drug delivery systems to manage OAB.
Mucoadhesion-based drug delivery systems have recently gained interest because of their bio-adhesion capability, which results in enhanced residence time leading to prolonged duration of action with the mucosal surface, potentially improving compliance and convenience. Mucoadhesion testing of these formulations is widely reported; however, this is technically challenging due to the absence of any standard methods and difficulty in conducting mucoadhesion, formulation-mucosal surface interaction, mucosal surface topography and drug release in a single experiment. As these measurements are currently conducted separately, on replicate formulations, results can often be subjective and difficult to correlate. Hence, the aim of the present study was to develop a new AFM-based single-entity ex vivo muco-dissolution (MUCO-DIS) technique to simultaneously evaluate mucoadhesion force, 3D surface topography, polymer dissolution and drug release characteristics. To demonstrate the potential of the current technique, the interactions between model pectin microparticles containing metformin HCl and a range of gastrointestinal mucosal surfaces (gastric, small intestine, large intestine and buccal) were studied. This novel system has not only successfully determined the mucoadhesion force, polymer dissolution and drug release information but has also highlighted the difference in microparticle performance with different mucosal targets. The current work has highlighted the potential of this newly developed MUCO-DIS system and we believe this will be a valuable tool for characterising these popular pharmaceutical formulations. This technique could also provide an opportunity to other scientific fields to evaluate materials, substrate behaviour and their interactions in their hydrated state at nanoscale with real-time chemical and surface mapping.
This study aims to explore the potential of gum extracted from okra fruit (Hibiscus esculentus) in developing hydrophilic matrices for controlled drug release applications, including determination of its percolation threshold. Flurbiprofen (poorly soluble), theophylline (sparingly soluble) and metformin (freely soluble) were employed as model drugs and incorporated using direct compression into matrices containing 40% w/w of three drugs with different physicochemical properties. Atomic force microscopy was used to study the surface texture properties of developed matrices; the surfaces of the flurbiprofen-based matrices were comparatively rough most likely as a consequence of its poor compactability. Swelling studies found that the swelling rate increased as the concentration of okra gum was increased. However, for all matrices, an increase in the gum concentration resulted in decreased drug release. The estimated percolation threshold of the okra gum calculated was found in the region of ~25% v/v plus initial porosity. Knowing the percolation threshold will enable formulators to use the minimal amount of polymer for sustain release matrices thus the controlling costs and maximising the sustainable potential of okra. This study will not only assist researchers in developing effective okra gum-based extended-release matrices but also expected to contribute towards its exploration at an industrial scale.
the present study aimed to explore a new source of montmorillonite and to develop an extraction and purification protocol for its isolation from raw clay samples acquired from the Koh-e-Suleiman mountain range in Pakistan. The process involved the collection of raw clay from the source, identification and quantification of montmorillonite. Granulometric extraction and purification protocols increased the montmorillonite content from 21.8-25.1% in the raw clay to 90.1-93.9% after small-scale extraction and 85.33-89.33% on a larger scale. A techno-economic analysis highlighted the practicality and economic benefits of large-scale extraction for industrial applications. This study highlights the existence of a substantial new source of this valuable clay which is currently used across multiple industries including construction, pottery making, pharmaceuticals, cosmetics and engineering. it is intuitively expected that the large-scale extraction of the material will improve the economic condition of the region by providing employment opportunities to locals and may be a valuable resource for export. The term clay generally refers to a natural material with plastic properties and particles or fragments of very fine size (<2 µm), composed mostly of hydrous-layer silicates of aluminium 1. Based on chemical composition and atomic structure, clays can be classified into four groups: kaolinite, illite, chlorite and smectite 2. As well as commonly known uses in construction and pottery making, their utilisation extends into multiple industries including pharmaceuticals, cosmetics, engineering and healthcare. The healing and medicinal properties of clays have long been recognised by humans and even animals, and other properties, such as high adsorption capacity, specific surface area, swelling capacity, reactivity to acids, dispersivity, hygroscopicity, unctuosity, thixotropy, plasticity and opacity, have led to their extensive and diverse range of applications 3-5. Montmorillonite clay has been identified as possessing desirable properties for exploitation across different industries, including pharmaceuticals, cosmetics, engineering and healthcare. It is a porous clay mineral belonging to the smectite group and is composed of a 2:1-layered structure with exchangeable cations between the layers 6. It has been widely studied as an active ingredient in pharmaceuticals due to its swelling, rheological, moisture-retaining, adsorption, detoxification and anti-viral properties 7-9. The adsorptive capacity of montmorillonite renders it suitable for drug entrapment and sustained-release, and its swelling and rheological properties
Overactive bladder (OAB) is a symptomatic complex condition characterised by frequent urinary urgency, nocturia, and urinary incontinence with or without urgency. Gabapentin is an effective treatment for OAB, but its narrow absorption window is a concern, as it is preferentially absorbed from the upper small intestine, resulting in poor bioavailability. We aimed to develop an extended release, intragastric floating system to overcome this drawback. For this purpose, plasticiser-free filaments of PEO (polyethylene oxide) and the drug (gabapentin) were developed using hot melt extrusion. The filaments were extruded successfully with 98% drug loading, possessed good mechanical properties, and successfully produced printed tablets using fused deposition modelling (FDM). Tablets were printed with varying shell numbers and infill density to investigate their floating capacity. Among the seven matrix tablet formulations, F2 (2 shells, 0% infill) showed the highest floating time, i.e., more than 10 h. The drug release rates fell as the infill density and shell number increased. However, F2 was the best performing formulation in terms of floating and release and was chosen for in vivo (pharmacokinetic) studies. The pharmacokinetic findings exhibit improved gabapentin absorption compared to the control (oral solution). Overall, it can be concluded that 3D printing technology is an easy-to-use approach which demonstrated its benefits in developing medicines based on a mucoadhesive gastroretentive strategy, improving the absorption of gabapentin with potential for the improved management of OAB.
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