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Fluconazole (FLZ) is the most widely used antifungal agent for treating cutaneous candidiasis. Although oral FLZ has been proved to be effective, the incidence of side effects necessitates the development of an effective formulation that could surpass the pitfalls associated with systemic availability. Accordingly, this research aimed at developing a self-assembled mixed micelles topical delivery system to enhance the topical delivery of the drug. Self-assembled mixed micelles were developed using D-α-tocopheryl polyethylene glycol 1000 succinate and phospholipids and optimized using Box-Behnken design. The optimized formulation with minimized size was then tested in vivo for the antifungal activity against C. albicans in immunocompromised mice. Treatment with the optimized formulation led to decreased peripheral erythema as well as lesions due to fungal infection in comparison to raw FLZ loaded gel. Therefore, the developed formulation was found to be a promising vehicle for the treatment of cutaneous candidiasis.

Magnolia bark is an important food supplement. Magnolol (ML), 3,3'-Neoligna-8,8'-diene-4,4'- diol, is a bioactive phenolic molecule found in the Magnolia family. Advanced Drug Delivery Systems (DDSs) have been able to enhance therapeutic efficacy and reduce adverse effects of plant-derived bioactive. In the first part of the review, the bioactivities, mechanisms, and clinical prospects of ML are described. A brief explanation of the mechanisms of anti-inflammatory, antioxidant, cardiovascular-protective, neuroprotective, and anti-cancer effects of ML is also provided. Later, the detailed biopharmaceutics of ML is described under solubility, dissolution, bioavailability, and pharmacokinetics. The solubility of ML in different media pH is also explained. The bioavailability of pure ML and its pharmacokinetics after parenteral and oral administrations are described. Further, pharmacokinetics after single and multiple doses of ML is also discussed. Finally, the reported advanced DDSs of ML are reviewed critically. Engineered crystals, solid dispersions, microstructures, and nanostructures of ML-loaded DDSs are reviewed. [ABSTRACT FROM AUTHOR]

Layered double hydroxides (LDHs) are highly effective drug delivery systems, owing to their capacity to intercalate or adsorb biomaterials, flexible structure, swelling property, high stability, good biocompatibility, and ease of synthesis. Phenytoin (PHT) is an antiseizure BCS (Biopharmaceutics Classification System) class II drug, presenting low aqueous solubility. Therefore, the current study aimed at increasing its solubility, dissolution, and bioavailability. PHT was intercalated to the MgAl-LDH formed in situ and successful intercalation to form MgAl-PHT-LDH was confirmed by FTIR, PXRD, DSC, and TGA. Examination of particle size and morphology (by photon correlation spectroscopy and electron microscopy, respectively) confirmed the formation and intercalation of nanostructured LDH. Intercalation enhanced the saturation solubility of PHT at 25°C in 0.1N HCl and phosphate buffer (pH 6.8) by 6.57 and 10.5 times respectively. The selected drug excipient powder blend for the formulation of MgAl-PHT-LDH tablets exhibited satisfactory properties in both pre-compression parameters (angle of repose, bulk density, tapped density, Carr's index, and Hausner ratio) and tablet characteristics (weight variation, thickness, hardness, friability, content uniformity, and disintegration time). MgAl-PHT-LDH tablets showed better dissolution of PHT compared to unprocessed PHT tablets at all time points. Oral bioavailability of MgAl-PHTLDH tablets and unprocessed PHT tablets was tested in two groups of Sprague Dawley rats based on analysis of serum levels of both forms of PHT by UPLC-ESIMS/MS serum. MgAl-PHT-LDH tablets demonstrated a relative bioavailability of 130.15% compared to unprocessed PHT tablets, confirming a significantly higher oral bioavailability of MgAl-PHT-LDH. In conclusion, MgAl-PHT-LDH could provide a strategy for enhancing solubility, dissolution, and thereby bioavailability of PHT, enabling the evaluation of theclinical efficacy of MgAl-PHT-LDH tablets for the treatment of seizures at lower PHT doses. [ABSTRACT FROM AUTHOR]

Introduction: Microorganisms originating from the marine environment, such as bacteria, fungi, and algae, are deliberately employed in the production of nanoparticles on account of the wide array of bioactive compounds they produce. Methods: Cell-free aqueous extracts of marine Bacillus subtilis (CBPPR1) were used to synthesise AuNPs (CBPPR1AuNPs) and AgNPs (CBPPR1AgNPs). Zetasizer Nano ZS (Malvern Instruments) zeta size and zeta potential, field emission and transmission scanning electron microscopy (FE-SEM and HR-TEM), UV-visible (UV-Vis), X-ray diffraction (XRD), Fourier transform infrared (FT-IR), and EDAX were used to characterize biogenically synthesized nanoparticles (NPs). Their antibacterial activities against Escherichia coli, Klebsiella pneumoniae, and Staphylococcus aureus were investigated. The anticancer efficacy of CBPPR1Au and AgNPs was investigated in human colorectal adenocarcinoma cell lines (HT-29, HT-116). CBPPR1AgNPs formulation was studied in vitro and invivo rat models. The assessment focused on its efficacy in wound healing and antibacterial capabilities, comparing them against a commercial product. To determine the effectiveness of CBPPR1AgNPs in wound healing, a cutaneous wound model was employed, which included infection with S. aureus. Results and discusion: CBPPR1Au and AgNPs significantly inhibited the growth of S aureus at MIC of 125 µg (CBPPR1AuNPs) and 62.5 µg (CBPPR1AgNPs) respectively. FE-SEM and HR-TEM observations confirmed that NPs caused bacterial cell leakage, damage, and shrinkage. Cancer cell viability was reduced upon treatment with increasing concentrations of CBPPR1Au and AgNPs, and apoptosis was increased in cells treated with CBPPR1Au and AgNPs relative to untreated cells (p < 0.001). CBPPR1Au and AgNPs showed significant cytotoxic activity against HT-29 (15.5 M) and HT-116 (62.5 M) cells. In-vivo experiments on rats showed minimal pus formation in groups CBPPR1AgNPs (62.5 µg/ml) G2, CBPPR1AgNPs (125 µg/ml) G3, and silver sulfadiazine G4, indicating the effective control of infections. CBPPR1AgNPs-treated wounds showed complete closure, whereas untreated G1 wounds remained unhealed. Histopathological analysis showed no adverse effects of CBPPR1AgNPs on kidneys and livers of rats. These findings suggest that CBPPR1AgNPs play a pivotal role in wound healing because of their potent antibacterial properties. [ABSTRACT FROM AUTHOR]

The present study aimed to develop diclofenac sodium nanoemulgel for managing pain and inflammation using the low-energy emulsification technique. Nanoemulsion of diclofenac was formulated using clove oil with adequate amount of surfactants and cosurfactants, and it was converted to hydrogel form using Carbopol 980 as the gelling agent. The droplet size of the oil globules in the nanoemulsion was found to be 64.07 ± 2.65 nm with a low polydispersity index (0.238 ± 0.02) along with high negative zeta potential (−39.06 mV). The developed nanoemulgel exhibited non-Newtonian and pseudoplastic behavior. The in vitro release profile of the developed nanoemulgel was higher as compared to marketed and conventional gel. The carrageenan-induced paw edema test was performed in rats to evaluate the anti-inflammatory activity of developed nanoemulgel. The developed nanoemulgel showed significantly higher (p < 0.01) effect in reducing pain and inflammation symptoms as compared to marketed as well as conventional gel of diclofenac. The overall findings of the study suggest that the developed nanoemulgel formulation of diclofenac can be used as a potential approach for the management of pain and inflammation. [ABSTRACT FROM AUTHOR]