Current Pharmaceutical Design - Volume 30, Issue 40, 2024

Clindamycin (CLIN), an antibiotic sold in the form of capsules, injectable solution, gel, and lotion, is easily soluble in water and ethanol. However, it lacks eco-efficient methods for evaluating pharmaceutical products.

The objective of this review is to provide an overview of the analytical methods present both in the literature and in official compendia for evaluating pharmaceutical matrices based on CLIN in the context of Green Analytical Chemistry (GAC).

Firstly, microbiological methods for evaluating the potency of CLIN final products were not found, which already shows the need to develop new methods. Among the methods found, which are all physical-chemical, the most used method is HPLC (71%) followed by UV-vis (14%). Among the targets of the methods, capsules and raw materials were the most studied (33% each). Among the choices of analytical conditions for the methods, acetonitrile is the preferred solvent (27.7%), even though CLIN is easily soluble in ethanol.

Thus, the gap in eco-friendly and sustainable analytical methods is a reality and an opportunity for analytical development centers to provide means for evaluating the quality of CLIN-based products.

The current investigation involved the development and application of a topical treatment for wound healing for sesamol loaded into the silver nanoparticles (SML-AgNPs).

SML-AgNPs were produced through the application of microwave technique. The SML-AgNPs were further optimized utilizing a Box-Behnken design (BBD).

The Opt-SML-AgNPs formulation that was optimized demonstrated a particle size of 160.49 ± 1.11 nm, a polydispersity index (PDI) of 0.241 ± 0.54, a zeta potential of -21.09 ± 0.88 mV, and an efficiency of 84.19 ± 1.19%. The morphology of the Opt-SML-AgNPs reveals a spherical structure. The Opt-SML-AgNPs exhibit a higher in vitro drug release rate as compared to the SML suspension. The Opt-SML-AgNPs were incorporated into the carbopol gel (Opt-SML-AgNPG) and evaluated for various parameters. The skin permeation investigation revealed a twofold increase for the Opt-SML-AgNPG formulation when compared to the SML-conventional gel formulation. This finding indicates a prolonged release pattern and an enhanced permeability profile. The Opt-SML-AgNPs formulation exhibited a higher level of antioxidant activity when compared to the SML solution which is beneficial for wound healing.

In conclusion, the Opt-SML-AgNPG exhibits considerable potential in effectively penetrating the deeper dermal layers. Therefore, it may be considered that they possess the potential to serve as a suitable nanocarrier to administer topical delivery in the context of treating skin-related illnesses.

Studies have confirmed that high dose borneol has perinatal toxicity and has a certain effect on embryonic development. However, there is little about the effect of borneol on the development of zebrafish embryos. Therefore, we compared the effects of D-borneol, L-borneol and synthetic borneol on the growth and development of zebrafish embryos, and predicted the possible mechanism of perinatal toxicity.

The embryonic mortality rate, hatching rate, and heart rate of each group were recorded at 48 hpf to compare the effects of borneols on the development of zebrafish embryos. Network pharmacology and molecular docking technology were used to predict the possible mechanism of perinatal toxicity.

We found that borneols increased the mortality at 24 and 48 hpf, inhibited the autonomous movement behavior at 24 hpf, and affected the hatching rate and heart rate at 48 hpf. Network pharmacology analysis showed that borneols had the same toxic targets in the perinatal period and were involved in regulating perinatal toxicity by regulating pathways in cancer, chemical carcinogenesis-receptor activation, PI3K-Akt and others. Molecular docking showed that the binding activity of the active ingredients and the core target was at a medium level, and the binding activity of the borneols active ingredients and the core target was not much different.

Three kinds of borneol on the development of zebrafish embryos were different. The toxicity of L-borneol was the lowest. The mechanisms of perinatal toxicity were related to inflammation, apoptosis, cell cycle and growth, differentiation and reproduction.

To examine the correlation between Atherogenic Index of Plasma (AIP) levels and the progression of non-target lesion vascular disease following the deployment of Drug-eluting Stents (DES).

We retrospectively enrolled patients who had undergone successful treatment for CAD with DES and subsequently underwent a coronary angiography follow-up at the Cardiology Department of Tianjin Third Central Hospital from January 2017 to July 2022. The annual change in Gensini Score (GS) was calculated according to two angiographic evaluations in order to assess the progression of non-target lesion vascular disease; a change greater than 1 indicated progression, while a change of 1 or less indicated stability. AIP was calculated according to serum lipid parameters. Multivariate Logistic regression model was used to evaluate the relationship between AIP level and progression of non-target coronary artery lesions. The ROC curve analysis was performed to evaluate the diagnostic value of AIP for coronary artery non-target lesion vascular disease progression.

Out of the 344 patients who were monitored over a median duration of 1.2 years, 113 exhibited progression of non-target lesion vascular disease. Initially, baseline AIP levels were notably higher in the progression group compared to the non-progression group (0.30 [0.14, 0.43] vs. 0.11 [-0.06, 0.31]), and this difference remained significant during the follow-up period (0.19 [0.06, 0.34] vs. 0.11 [-0.06, 0.22]). Multivariate logistic regression revealed that AIP is an independent predictor for the progression of non-target lesion vascular disease following DES treatment. Individuals in the highest tertile of AIP faced a considerably elevated risk compared to those in the lowest tertile (OR = 4.88, 95% CI: 2.12-11.21, P < 0.001). Moreover, utilizing receiver operating characteristic curve analysis, a 0.15 AIP level cut-off was determined for diagnosing disease progression, with a sensitivity of 73.5% and specificity of 56.7%, and an area under the curve of 0.672 (95% CI: 0.613-0.731, P < 0.01).

AIP significantly correlates with the progression of non-target lesion vascular disease among patients with coronary artery disease who have undergone DES treatment, establishing itself as an independent risk factor in addition to conventional predictors.

This study aimed to prepare, characterize, and in vitro and in vivo evaluate a novel nanostructured lipid carriers (NLCs) formulation containing two fractions of Glycyrrhiza glabra L. (licorice) extract for the treatment of hyperpigmentation.

Two fractions, one enriched with glabridin (FEG) and the other enriched with liquiritin (FEL), were obtained by partitioning the methanol (MeOH) extract of licorice roots with ethyl acetate (EtOAc) and partitioning the EtOAc fraction with butanol (n-BuOH) and water. The quantities of glabridin (Glab) and liquiritin (LQ) in the fractions were determined by high-performance liquid chromatography (HPLC). FEG and FEL were loaded in different NLC formulations, and surface characterization and long-term stability were studied using dynamic light scattering (DLS). The best formulation was chosen for further surface characterization, including transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and fourier-transform infrared (FTIR) spectroscopy. Moreover, entrapment efficiency percentage (EE%), in vitro drug release, in vivo skin penetration, cytotoxicity on B16F10 melanoma cells, effect on melanin production, and anti-tyrosinase activity were tested for the selected formulation.

Based on HPLC results, FEG contained 34.501 mg/g of Glab, and FEL contained 31.714 mg/g of LQ. Among 20 different formulations, NLC 20 (LG-NLCs) showed desirable DLS results with a Z-average size of 185.3 ± 1.08 nm, polydispersity index (PDI) of 0.229 ± 0.35, and zeta potential of -16.2 ± 1.13 mV. It indicated good spherical shape, high EE% (79.01% for Glab and 69.27% for LQ), two-stage release pattern (an initial burst release followed by sustained release), efficient in vivo skin penetration, and strong anti-tyrosinase activity. LG-NLCs had acceptable physiochemical stability for up to 9 months and were non-cytotoxic.

The LG-NLC formulation has revealed desirable surface characterization, good physiochemical stability, efficient drug release pattern and in vivo penetration, and high EE%. Therefore, it can be a suitable nanosystem for the delivery of licorice extract in the treatment of hyperpigmentation.