The major goal of this investigation was to prepare carvedilol nanocrystals (CRL-NCs) for better solubility, stability, and bioavailability. Using polyvinyl pyrolidine K-30 (PVP) and sodium dodecyl sulphate (SDS) as stabilisers, CRL-NCs were effectively synthesised by emulsion-diffusion, followed by the high-pressure homogenization (HPH) method. The AL classes of phase solubility curves with ideal complexes produced with stabilisers were estimated by thermodynamic parameters. The docking study was performed with the active site of a β-1 adrenoreceptor protein, and the CRLs docking score was revealed as −23.481 Kcal/mol−1. At 25 and 37 °C, the optimum interaction constant was determined for PVP (144 and 176 M−1) and SDS (102 and 121 M−1). The average particle size (PS) of the produced stable CRL-NCs is 58 nm, with a zeta potential of −27.2 ± 2.29 mV, a poly dispersibility index of 0.181 ± 0.012, a percentage yield of 78.7 ± 3.41, drug content of 96.81 ± 3.64%, and entrapment efficiency of 83.61 ± 1.80%. The morphological data also reveals that the CRL-NCs were nearly sphere shaped, with distinct and smooth surfaces. CRL-NCs were studied using X-ray diffraction (XRD), fourier transform infrared (FT-IR) spectroscopy, and differential scanning calorimetry (DSC), and the results show no chemical structural alterations, even when PS was reduced. NCs accelerate their in vitro dissolution release rate by about three times faster than CRL-MCs (microcrystals). When kept at 4 °C, the CRL-NCs exhibit good physical stability for six months. As a result, the CRL-NCs created via emulsion-diffusion followed by HPH with stabilisers can be used to increase the solubility, stability, and bioavailability of poorly soluble or lipophilic drugs.
This paper reports the antifungal properties of zinc oxide nanoparticles (ZnO NPs) on Candida albicans ATCC 1023 through the study of growth inhibitory effects of ZnO NPs on C. albicans and the effect of the nanoparticles on the surface of C. albicans. The growth inhibitory effects of ZnO NPs (5, 10, 20, 40, 80, and 160 µg/mL) on C. albicans at 24 h were determined through the reduction in suspension turbidity and colony count. Fourier transform infrared (FTIR) analysis was carried out to establish the functional groups associated with the interaction of ZnO NPs on the yeast cell wall, while scanning electron microscopy (SEM) with energy dispersive X-ray (SEM-EDX) analysis was utilised to determine the surface accumulation of ZnO NPs on the yeast cells and the consequential morphological alterations on C. albicans. The results exhibited a significant (p < 0.05) growth inhibition for all tested concentrations except for 5 µg/mL of ZnO NPs at 24 h as compared to negative control. FTIR analysis revealed the possible involvement of alcohol, amide A, methyl, alkynes, amide I and II, and phosphate groups from the yeast cell wall of C. albicans in the surface interaction with the ZnO NPs. Finally, SEM-EDX revealed a considerable accumulation of ZnO NPs on the yeast cells and consequential morphological alterations on C. albicans, including the damage of hyphae, pitting of the cell wall, invagination, and rupture of the cell membrane. The current study demonstrated that ZnO NPs possess antifungal properties against C. albicans in a dose-dependent manner, and the surface interaction of ZnO NPs on fungal cells caused alterations in cell membrane integrity that might have resulted in cell death.
Transferosomes are one of the vesicular carriers that have received extensive research and attention recently because of their capacity to get beyond the barriers posed by the stratum corneum to penetration. The intent of the current study is to optimize and evaluate proanthocyanidin (PAC) containing transferosomal transdermal gels. PAC-containing transferosomes were prepared using the film hydration method and then loaded into a 4% methylcellulose gel. A 23 Box–Behnken design was used to optimize the PAC-loaded transferosomal gel, where the effects of phospholipid 90 G (X1), Tween 80 (X2), and sonication time (X3) were evaluated. The formulation factors, such as the drug entrapment efficiency percentage (PEE) and in vitro drug release, were characterized. A PEE of 78.29 ± 1.43% and a drug release in vitro at 6 h of 24.2 ± 1.25% were obtained. The optimized transferosomal-loaded proanthocyanidin (OTP) formulation penetrated the porcine skin at an excellent rate (0.123 ± 0.0067 mg/cm2/h). Stability tests were conducted for OTP to predict the effects of various temperature conditions on the physical appearance, drug content, and PEE for periods of 15, 30, and 45 days. Finally, this transferosomal system for transdermal PAC delivery may be a suitable alternative to the conventional treatment for osteoarthritis.
Antimicrobials are widely used to treat bacteria, viruses, fungi, and protozoa. Therefore, research and development of newer types of antimicrobials are important. Antimicrobial resistance has emerged as a major challenge to the healthcare system, although various alternative antimicrobials have been proposed. However, none of these show consistent and comparable efficacy to antimicrobials in clinical trials. More recently, nanoparticles have emerged as a potential solution to antimicrobial agents to overcome antimicrobial resistance. This article revisits and updates applications of various types of nanoparticles for the delivery of antimicrobial agents and their characterization. Though nanoparticle technology has some limitations, it provides an innovative approach to pharmaceutical technology. Furthermore, nanoparticles offer a variety of advantages, such as enhancement of solubility and permeation, leading to better efficacy. In this article, approaches commonly employed to improve antimicrobial therapy are discussed. These approaches have advantages and applications and provide a broader opportunity for pharmaceutical scientists to choose the proper method per the desired outcome.
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