The dawning era of oral thin films for nutraceutical delivery: From laboratory to clinic.

Oral thin films (OTFs) are innovative dosage forms that have gained tremendous attention for the delivery of nutraceuticals. They are ultra-thin, flexible sheets that can be easily placed on the tongue, sublingual or buccal mucosa (inner lining of the cheek). These thin films possess several advantages for nutraceutical delivery including ease of administration, rapid disintegration, fast absorption, rapid onset of action, bypass first-pass hepatic metabolism, accurate dosing, enhanced stability, portability, discreetness, dose flexibility and most importantly consumer acceptance. This review highlights the utilization OTFs for nutraceutical delivery, their composition, criteria for excipient selection, methods of development and quality-based design (QbD) approach to achieve quality product. We have also provided recent case studies representing OTFs as promising platform in delivery of nutraceuticals (plant extracts, bioactive molecules, vitamins, minerals and protein/peptides) and probiotics. Finally, we provided advancement in technologies, recent patents, market analysis, challenges and future perspectives associated with this unique dosage form.

Preparation, Characterization, and Antioxidant Activity of L-Ascorbic Acid/HP-ß-Cyclodextrin Inclusion Complex-Incorporated Electrospun Nanofibers.

L-Ascorbic acid (LAA) is a key vitamin, implicated in a variety of physiological processes in humans. Due to its free radical scavenging activity, it is extensively employed as an excipient in pharmaceutical products and food supplements. However, its application is greatly impeded by poor thermal and aqueous stability. Herein, to improve the stability and inhibit oxidative degradation, we prepared LAA-cyclodextrin inclusion complex-incorporated nanofibers (NFs). The continuous variation method (Job plot) demonstrated that LAA forms inclusions with hydroxypropyl-ß-cyclodextrin (HP-ß-CD) at a 2:1 molar stoichiometric ratio. The NFs were prepared via the single step electrospinning technique, without using any polymer matrix. The solid-state characterizations of LAA/HP-ß-CD-NF via powder x-ray diffractometry (PXRD), Fourier-transform infrared (FT-IR) analysis, differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), and nuclear magnetic resonance (1H NMR and 2D-NOESY) spectroscopy, reveal the effective encapsulation of the LAA (guest molecule) inside the HP-ß-CD (host) cavity. The SEM micrograph reveals an average fiber diameter of ~339 nm. The outcomes of the thermal investigations demonstrated that encapsulation of LAA within HP-ß-CD cavities provides improved thermal stability of LAA (by increasing the thermal degradation temperature). The radical scavenging assay demonstrated the enhanced antioxidant potential of LAA/HP-ß-CD-NF, as compared to native LAA. Overall, the study shows that cyclodextrin inclusion complex-incorporated NFs, are an effective approach for improving the limitations associated with LAA, and provide promising avenues in its therapeutic and food applications.

Role of Divalent Cations in HIV-1 Replication and Pathogenicity.

Divalent cations are essential for life and are fundamentally important coordinators of cellular metabolism, cell growth, host-pathogen interactions, and cell death. Specifically, for human immunodeficiency virus type-1 (HIV-1), divalent cations are required for interactions between viral and host factors that govern HIV-1 replication and pathogenicity. Homeostatic regulation of divalent cations' levels and actions appear to change as HIV-1 infection progresses and as changes occur between HIV-1 and the host. In people living with HIV-1, dietary supplementation with divalent cations may increase HIV-1 replication, whereas cation chelation may suppress HIV-1 replication and decrease disease progression. Here, we review literature on the roles of zinc (Zn2+), iron (Fe2+), manganese (Mn2+), magnesium (Mg2+), selenium (Se2+), and copper (Cu2+) in HIV-1 replication and pathogenicity, as well as evidence that divalent cation levels and actions may be targeted therapeutically in people living with HIV-1.