Drug Delivery Letters - Volume 13, Issue 2, 2023

Coronavirus disease (COVID-19) is an infectious disease caused by coronavirus. Developing specific drugs for inhibiting replication and viral entry is crucial. Several clinical trial studies are underway to evaluate the efficacy of anti-viral drugs for COVID-19 patients. Nanomedicine formulations can present a novel strategy for targeting the virus life cycle. Nano-drug delivery systems can modify the pharmacodynamics and pharmacokinetics properties of anti-viral drugs and reduce their adverse effects. Moreover, nanocarriers can directly exhibit anti-viral effects. A number of nanocarriers have been studied for this purpose, including liposomes, dendrimers, exosomes and decoy nanoparticles (NPs). Among them, decoy NPs have been considered more as nanodecoys can efficiently protect host cells from the infection of SARS-CoV-2. The aim of this review article is to highlight the probable nanomedicine therapeutic strategies to develop anti-viral drug delivery systems for the treatment of COVID-19.

Aim: The present study evaluates the feasibility of the incorporation of palmitoylated arabinogalactan in solid lipid nanoparticles and its potential as a hepatospecific targeting ligand. Background: Human hepatocellular carcinoma (HCC) is a neoplasm presenting low survival and higher incidence, due to difficulties in the treatment modalities to effectively place cancer therapeutics at the site. Targeting asialoglycoprotein receptors on the surface of hepatocytes employing lipid nanoparticles, and liposomes presents opportunities for improvement in therapy. Objective: The objective of the present investigation was to fabricate and evaluate the potential of palmitoylated arabinogalactan (PAG) incorporated SLNs to target asialoglycoprotein receptors. Methods: Daunorubicin-loaded targeted SLNs prepared by ultrasound dispersion method were evaluated for in vitro release and in vitro cytotoxicity. Lipids, surfactants, and biocompatible solvents were screened for SLN formation and optimization was done using 2² factorial designs. Results: The particle size for formulations was below 200 nm with a unimodal distribution. Differential scanning calorimetry analysis revealed the interaction of lipids with other components characterized by a shift in lipid melting endotherm. Daunorubicin-loaded PAG SLNs released a significantly higher amount of daunorubicin at pH 5.5 as compared to pH 7.4, providing an advantage for targeted tumor therapy. In vitro cytotoxicity studies showed that daunorubicin depicted a dosedependent reduction in viability in all cell lines treated with formulation as well as free drug. Conclusion: SLNs showed enhancement in intracellular uptake of daunorubicin thereby establishing their potential in improved treatment of HCC and warrant further in vivo investigations.

Background : The prime intent of this study was to formulate, optimize and evaluate the floating microballoons of rosuvastatin calcium to extend the stomach or gastrointestinal residence time, dissolution rate, and bioavailability of the drug. 

Objective : Formulation development, statistical optimization, in vitro and in vivo characterization of floating microballoons of rosuvastatin calcium for cardiovascular diseases with improved dissolution rate, solubility, and bioavailability potential were the main objectives of this study. 

Background: Alzheimer’s is one of the primary causes and the most prevalent form of age-related dementia worldwide. There is an urgent surge to find an effective treatment for AD due to its social implications on society. Aim: Present research work aims to develop Chitosan nanoparticles of leuprolide acetate for the treatment of Alzheimer’s disease by delivery through the intranasal route. Methods: Chitosan nanoparticles encapsulating leuprolide acetate were prepared using the ionic gelation method and optimized using a central composite design. The optimized nanoparticles were evaluated by DSC study, TEM analysis, release study of the drug in vitro and ex vivo, histopathology study, and accelerated stability study, In vivo kinetic and dynamic study. Results: The optimized formulation exhibited particle size of 254.3 ± 10.7 nm, % EE of 85.6 ± 0.8 %, and zeta potential of +18.0 ± 0.2 mv. The release of drug from optimized nanoparticles in vitro was in a sustained manner, with only 75.7 % drug released at 48 hours. Higher permeation of the drug from nanoparticles (Papp =5.44 ± 0.34 x 104) was observed in the diffusion study ex vivo. Sheep nasal toxicity and accelerated stability study proved the intranasal safety and stability of the developed formulation. The in vivo drug uptake study indicated a greater brain drug concentration from chitosan nanoparticles than from plain drug solution. The anti-Alzheimer potential was also evident from behavioural studies and histopathology study of rat brain. Conclusion: Thus, the chitosan nanoparticulate formulation of leuprolide acetate was found to have great potential for Alzheimer’s disease management.

Background: Conventional administration of chemotherapeutic agents associated with low drug distribution to cancer cells with multiple systemic toxicities. Thus, enhancing the active delivery of chemotherapeutic agents to cancer cells increases drug distribution and internalization to targeted cells with minimal systemic toxicities. Objective and Aim: The current study was designed to prepare and optimize solid lipid nanoparticles (SLN) containing stearic acid (SA) that mediate active delivery and uptake of gefitinib (GEF) to cancer cells. Methods: The stability of the prepared Plain-SLN formulations was characterized for 90 days. The most stable formulations were loaded with GEF (GEF-SLN) and subjected to pharmaceutical characterization. In vitro dissolution of GEF-SLN formulations was studied using the dialysis method. Biosafety in the terms of hemocompatibility was investigated using fresh blood samples. Additionally, the cytotoxicity of GEF-SLN was examined against the lung cancer cell line (A549). Results: The obtained results showed that the prepared formulations fall in the nanosize range from 114 to 411 nm with a negative zeta-potential value from -17 to -27 mV. The particle size of Plain- SLN formulations was increased when the GEF is incorporated during preparation. Besides, the crystallinity of SA was disordered following the incorporation of GEF. In addition, GEF entrapment efficiency into SLN was 88% with a sustained-release profile of about 75% in 24 h. Additionally, the present results revealed that using surfactants with high drug solubility negatively impacts the stability of SLN formulation. Furthermore, hemocompatibility results revealed that all SLN formulations showed insignificant hemolysis (1- 4%) at all concentrations. Moreover, cytotoxicity examinations revealed that SLN enhanced the antiprofilated activity of GEF compared to free GEF. Conclusion: These data concluded that SLN is a hopeful approach to enhancing the selective deposition of GEF into cancer cells and reducing the lymphatic metastasis of lung cancer.

Aim/ Objective: The present investigation aims to develop a solid Self-nano emulsifying Drug Delivery System for enhancing the solubility and in vitro characteristics of poorly soluble anti- hypertensive drug Bosentan Monohydrate. Methods: The selection of formulation components on the basis of equilibrium solubility and pseudo- ternary phase titration studies revealed the suitability of Isopropyl myristate, Tween 80 and Polyethylene glycol as the lipidic excipients and their optimized concentration ranges resulted in a stable microemulsion region. Results: The systematic optimization of the liquid SNEDD formulations of Bosentan was performed using in vitro tests and detailed characterization studies. The results revealed that the F4 formulation produces excellent results and satisfactory results in all the CQA of liquid SNEDDS. The optimized liquid SNEDD formulations exhibited globule size of less than 100 nm, high and negative values of zeta potential, quick self-emulsification rate, negligible phase separation, and a high degree of physical stability during thermodynamic evaluation studies. SEM revealed nanostructured particles with negligible aggregation. Conclusion: In vitro dissolution studies of Bosentan in optimized liquid SNEDDS (F4) unveiled a multi-fold enhancement in release profile, as compared to pure API.