A Logical Approach to Development of Natamycin Loaded NLCs: Preformulation Studies, Formulation Development and In Vitro Characterization

This study was aimed at the development of natamycin loaded nano-structured lipid carriers (NLCs) and their characterization for physicochemical properties i.e., Fourier Transform Infrared (FTIR), UV-Visible spectroscopy, meting point, solubility profile and partition coefficient. FTIR and Differential Scanning Calorimetry (DSC) permit the characterization of the drug, excipients and binary mixture and thus assisted in predicting the compatibility of natamycin with other excipients. Lipid screening for formulation of NLCs were performed by their solubility and drug affinity studies. High homogenization and sonication method was employed for the development of natamycin loaded NLCs and it was characterized for vesicle size, zeta potential, % entrapment efficiency, viscosity, pH and percentage drug release up to 12 h.

Formulation Development of Nifedipine through Nanotechnology: A Comprehensive Review

Background: The therapeutic use of nifedipine, a dihydropyridine calcium channel blocker, is limited due to its poor solubility profile, rapid onset of its action, and short biological half-life. Many formulation techniques have been applied to improve the properties of the drug. Objective: The objective of the study is to summarize the nanotechnology approaches designed to improve the therapeutic and pharmacokinetic properties of nifedipine till 2020. Methods: The related articles were searched until 28th March, 2020, with the specific keywords, in Pubmed and google scholar, excluding review articles. Results: The discussion showed that among the nano-carriers used to improve the pharmacological property of the drug, lipid nanoparticles, polymeric nanoparticles, crystalline nanoparticles, and nano-emulsions have been used widely. Nanotechnology has been found efficient in improving the solubility profile of nifedipine, achieving sustained and controlled release, and achieving targeted and local delivery and transdermal drug delivery. By exploiting nano-formulations, new windows of therapeutic applications can be achieved. Furthermore, micelle media, polymeric nanoparticles, and microcrystalline nanoparticles have been used to develop a photostable formulation. Conclusion: The technological innovations in the field of nanomedicine have paved many ways for delivering nifedipine and such sparingly water-soluble compounds.

Hydrophilic or Lipophilic Statins?

Drugs can be classified as hydrophilic or lipophilic depending on their ability to dissolve in water or in lipid-containing media. The predominantly lipophilic statins (simvastatin, fluvastatin, pitavastatin, lovastatin and atorvastatin) can easily enter cells, whereas hydrophilic statins (rosuvastatin and pravastatin) present greater hepatoselectivity. Although the beneficial role of statins in primary and secondary cardiovascular prevention has been unequivocally confirmed, the possible superiority of one statin or other regarding their solubility profile is still not well-established. In this respect, although some previously published observational studies and clinical trials observed a superiority of lipophilic statins in cardiovascular outcomes, these results could also be explained by a greater low-density lipoprotein cholesterol reduction with this statin type. On the other hand, previous studies reported conflicting results as to the possible superiority of one statin type over the other regarding heart failure outcomes. Furthermore, adverse events with statin therapy may also be related to their solubility profile. Thus, the aim of the present review was to collect clinical evidence on possible differences in cardiovascular outcomes among statins when their solubility profile is considered, and how this may also be related to the occurrence of statin-related adverse effects.

β-Cyclodextrin/Isopentyl Caffeate Inclusion Complex: Synthesis, Characterization and Antileishmanial Activity

Isopentyl caffeate (ICaf) is a bioactive ester widely distributed in nature. Our patented work has shown promising results of this molecule against Leishmania. However, ICaf shows poor solubility, which limits its usage in clinical settings. In this work, we have proposed the development of an inclusion complex of ICaf in β-cyclodextrin (β-CD), with the aim to improve the drug solubility, and thus, its bioavailability. The inclusion complex (ICaf:β-CD) was developed applying three distinct methods, i.e., physical mixture (PM), kneading (KN) or co-evaporation (CO) in different molar proportions (0.25:1, 1:1 and 2:1). Characterization of the complexes was carried out by thermal analysis, Fourier-transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM) and molecular docking. The ICaf:β-CD complex in a molar ratio of 1:1 obtained by CO showed the best complexation and, therefore, was selected for further analysis. Solubility assay showed a marked improvement in the ICaf:β-CD (CO, 1:1) solubility profile when compared to the pure ICaf compound. Cell proliferation assay using ICaf:β-CD complex showed an IC50 of 3.8 and 2.7 µg/mL against L. amazonesis and L. chagasi promastigotes, respectively. These results demonstrate the great potential of the inclusion complex to improve the treatment options for visceral and cutaneous leishmaniases.

Synthesis and Characterization of 1-phenyl-3-methyl-4-stearoylpyrazol-5-one and Its Lanthanum(III) and Tungsten(VI) Complexes

The ligand, 1-phenyl-3-methyl-4-stearoylpyrazol-5-one (HSPy), and its La(III) and W(VI) complexes were synthesized and characterized spectroscopically using elemental analysis, UV-visible, IR, 1H and 13C NMR. Physical properties such as colour, melting points, conductivity measurements and solubility profile were also investigated. La(III) and W(VI) reacted with the ligand in the metal-ligand mole ratios of 1:3 and 1:2 to form neutral complexes of diaquo-trischelate La(SPy)3.2H2O and dioxoaquo-bischelate, WO2(SPy)2.H2O respectively.