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Chronotherapy of arthritis that is to reduce the early morning pain in the joints using pH sensitive hydrogel microspheres for colon targeting is a novel approach. Novel ketoprofen‐loaded pH‐sensitive Gellan gum‐Sodium alginate (Gg‐NaAlg) microspheres were developed by emulsion crosslinking method using Ethylene glycol dimethacrylate (EGDMA) as a crosslinker. The formulations were characterized by Scanning Electron Microscopy (SEM), Fourier Transforms Infrared Spectroscopy (FT‐IR), and Thermogravimetry. The influence of process parameters such as particle size distribution, drug encapsulation efficiency and matrix swelling has been investigated. The average particle size of microspheres varied from 50 to 100 μm giving an encapsulation efficiency of 70 %. Due to the pH‐sensitive swelling nature of microspheres, the drug was released in the colonic medium of pH of 7.4, but almost no release in acidic media. The kinetics of drug release was analyzed using empirical equations to understand the transport of drugs through polymeric matrices. Drug release was extended up to 10 hr and pulsatile release was observed depending upon the variation in the pH from stomach to colon region. [ABSTRACT FROM AUTHOR]

In the United States and Europe, the drug Memantine, Food and Drug Administration (FDA) approves a partial antagonist of the N-methyl-d-aspartate receptor (NMDAR), for the treatment of Alzheimer's disease (AD). Memantine may also be useful in treating other neurological disorders, such as dementia and Parkinson's disease (PD). As a neuroprotectant, memantine has been shown to have a favourable effect on both neurodegenerative and vascular processes in animal studies. Memantine--a partial NMDAR antagonist--blocks NMDA glutamate receptors to regulate the glutamatergic system and ease cognitive and memory issues while large quantities of glutamate induce neurodegeneration. For memantine to be effective, it must connect with the NMDAR in an uncompetitive manner, allowing the receptor's physiological function to be preserved while also ensuring that memantine is safe and has a low adverse-event profile. It's possible that memantine might be beneficial in the treatment of Parkinson's disease, since NMDAR antagonism has been implicated in the disease's pathophysiology, and no other medicine is effective enough to replace L-dopa. In spite of its mild side effects, memantine has only been demonstrated to produce a slight reduction in AD and VD, and hence attempts are being made to build new and more powerful memantine-based medications to perhaps provide higher effectiveness. In June 2021, the FDA authorized Aducanumab for medicinal use in the United States. The first-of-its-kind therapy for Alzheimer's disease and the first novel treatment for Alzheimer's since 2003 have been authorised by the FDA. [ABSTRACT FROM AUTHOR]

Researchers wanted to develop skin liposomal formulations that would carry 5-fluorouracil to the cancer site in an adjuvant way, as well as enhancing the health of basal cell carcinoma patients who were experiencing unfavorable consequences. Using Strat-M films in vitro, the detailed skin-damaging potential of the synthesized skin liposomes and the sensitivity to 5-fluorouracil were evaluated. It was found that the Korsmeyer-Pepas condition was the best one for controlling drug administration. Additionally, it is unknown if it might irritate skin. The vitality and hemolytic potential of the cytostatic effect on the recommended anti-tumor therapy were also examined in in vitro investigations. Our findings suggest that a sodium alginate and hyaluronic acid crosslinked gel containing AS1411 aptamer liposomes coated with 5-fluorouracil is the optimal liposome solution. This liposome characterization appears to have good biological safety implications and may be exploited as a different approach to basal cell carcinoma skin treatments. [ABSTRACT FROM AUTHOR]

In order to achieve increased felodipine delivery via transdermal delivery, the study investigated the parameters for improving various membrane combinations that incorporate lecithin derived from soy and eggs, in addition to an edge activator. This was done in order to achieve increased transdermal delivery. The Components and the Processes An approach known as rotational evaporation sonication was used in order to bring about the creation of a tranfersomal formulation. All of the following aspects of the formulation were evaluated and analysed: the polydispersity index, also known as the PDI, the zeta potential, the efficacy of trapping and loading, the deformability index, and in vitro skin penetration. Results: It was discovered that the best formulation would consist of spherical nanovesicles with a size of 75.71 5.4 nm, a PDI of 0.228, and a zeta potential of 49.8. (MF8). The fact that MF8's deformability index is so high—119.68—suggests that it attained the maximum degree of loading efficiency and entrapment possible. As compared to the transdermal control formulation, MF8's in vitro permeation through rat skin showed a 256% increase in permeability (flux = 23.72 0.64), with zero-order kinetics. This was in contrast to the transdermal control formulation, which improved permeability.This was determined by comparing the results to the transdermal control formulation (Case-II). Studies on the pharmacokinetics of the drug indicated that when transdermal therapy was compared to oral administration, the transdermal treatment resulted in a generally stable and maintained blood concentration with low plasma change, as well as a rapid and prolonged peak duration. The findings of confocal laser scanning microscopic studies, which showed that the medication quickly penetrated through dermal layers, were compatible with the relative bioavailability of felodipine, which was found to be 358.42% compared to oral administration. The results demonstrate that felodipine-loaded transfersomes are transcendent because they show that modifying the composition and manufacturing process had a significant influence on the features of the vesicles. [ABSTRACT FROM AUTHOR]

Novel Prednisolone sodium phosphate loaded hydrolyzed acrylamide grafted polyvinyl alcohol (Hy-PVA-g- AAm) microspheres were fabricated by using spray drying method. The primary objective of the work was to synthesize Hy-PVA-g-AAm with pH dependent swelling and its microspheres. The microspheres were evaluated by scanning electron microscopy (SEM) as well as fourier-transform infrared spectroscopy (FTIR). The influence of processing conditions on particle size, drug entrapment efficiency and swelling behaviour of the developed microspheres were studied. The microspheres were filled in enteric coated hard gelatine capsules to carry out the dissolution. The average particle size of the microspheres varied between 60-100 µm and the entrapment efficiency ranged between 84 to 94%. The microspheres exhibited pH responsive swelling with appreciably high swelling under colonic pH of 7.4 compared to acidic condition. The microspheres exhibited drug release in pH dependent manner. The cumulative percent drug release was found to be less than 20% in slightly acidic pH 6.8 resembling intestine and comparatively higher drug release in pH 7.4. The formulation followed Korsemeyer-Peppas kinetics with Non-Fickian diffusion after an adequate lag period. [ABSTRACT FROM AUTHOR]

Formulation and evaluation of oral dispersible film of domperidone was used as the primary objective of the present work, in order that can be successfully used for the management of emesis. In the work done, the films were prepared by solvent casting technique and in vitro performance was evaluated by the usual pharmacopoeial and unofficial tests. The oral dispersible film formed was found to be disintegrated within 1 minute. The thickness, drug content, tensile strength, surface pH, disintegration time (DT), mouth dissolving time and release profile of oral dispersible films were evaluated, and the best results were obtained at the formulation F3 containing Hydroxypropyl Methylcellulose (HPMC) E5 LV (100 mg), citric acid (20 mg), aspartame (5mg) and Polyethylene glycol (PEG)-400. The Formulation F3 showed 100.11% release within 10 minutes. As follows, the developed oral dispersible film of domperidone might be clinically used for fast release of drug in mouth, for better drug utilization and improved patient compliance. [ABSTRACT FROM AUTHOR]