In recent years, disease treatment has evolved strategies that require increase in pharmaceutical agent’s efficacy and selectivity while decreasing their toxicity in normal tissues. These requirements have led to the development of nanoscale liposome systems for drug release. This review focuses on lipid features, pharmacological properties of liposomal formulations and the clinical studies of their application. Several lipids are available, but their properties could affect pharmacological or clinical efficiency of drug formulations. Many liposomal formulations have been developed and are currently on the market. Proper selection of lipid is essential for the pharmacological effect to be improved. Most of the formulations use mainly zwitterionic, cationic or anionic lipids, PEG and/or cholesterol, which have different effects on stability, pharmacokinetics and delivery of the drug formulation. Clinical trials have shown that liposomes are pharmacologically and pharmacokinetically more efficient than drug-alone formulations in treating acute myeloid leukemia, hepatitis A, pain management, ovary, gastric breast and lung cancer, among others. Liposomal formulations are less toxic than drugs alone and have better pharmacological parameters. Although they seem to be the first choice for drug delivery systems for various diseases, further research about dosage regimen regarding dose and time needs to be carried out.

/pdf/nanomedicine-review-clinical-developments-in-liposomal-4x3c8c7qhb.pdf

Nanomedicine review: clinical developments in liposomal applications

The identification of MPTP, a relatively simple compound which causes selective degeneration of the substantia nigra after systemic administration, has had an a significant impact on the understanding and treatment of Parkinson’s disease (PD) over the last 30 years. This article is prefaced by the intriguing “medical detective story” that lead to the discovery of the biological effects of MPTP in humans. The steps that lead to the unraveling its mechanism of action and their impact on research into pathways underlying nigrostriatal degeneration are reviewed. The impact of the animal models that have been developed utilizing MPTP is also described with a focus on the translational implications of MPTP-related research. These include use of MAO-B inhibitors aimed at neuroprotection in PD and the importance of a stable primate model for PD which was utilized to better understand the circuitry of the basal ganglia, and the identification of the subthalamic nucleus as a target for deep brain stimulation. Finally, the results of a broad range of epidemiologic studies aimed as assessing the impact of environmental factors in PD that have been inspired by MPTP are summarized, including the discovery of other neurotoxicants (rotenone and paraquat) with parkinsonogenic effects. Overall, this article attempts to describe how the discovery of this nigral neurotoxicant began, where it is currently, and what the future may hold.

The MPTP Story.

Paclitaxel: What has been done and the challenges remain ahead.

The battle of “nano” paclitaxel

Taxol®, which is also known as paclitaxel, is a chemotherapeutic agent widely used to treat different cancers. Since the discovery of its antitumoral activity, Taxol® has been used to treat over one million patients, making it one of the most widely employed antitumoral drugs. Taxol® was the first microtubule targeting agent described in the literature, with its main mechanism of action consisting of the disruption of microtubule dynamics, thus inducing mitotic arrest and cell death. However, secondary mechanisms for achieving apoptosis have also been demonstrated. Despite its wide use, Taxol® has certain disadvantages. The main challenges facing Taxol® are the need to find an environmentally sustainable production method based on the use of microorganisms, increase its bioavailability without exerting adverse effects on the health of patients and minimize the resistance presented by a high percentage of cells treated with paclitaxel. This review details, in a succinct manner, the main aspects of this important drug, from its discovery to the present day. We highlight the main challenges that must be faced in the coming years, in order to increase the effectiveness of Taxol® as an anticancer agent.

https://www.mdpi.com/1420-3049/25/24/5986/pdf

A Compressive Review about Taxol®: History and Future Challenges

Antitumor effect and toxicity of Lipusu in rat ovarian cancer xenografts.

Protection of MPTP-induced neuroinflammation and neurodegeneration by rotigotine-loaded microspheres.

Acetylcholinesterase inhibitors (AChEIs), including Huperzine A (HupA), have been the mainstay of treatment for Alzheimer's disease (AD). However, AChEIs can cause gastrointestinal side effects, which has been related to the high Cmax and short tmax after oral administration. Clinical trials have verified that extended-release formulation with lower Cmax and prolonged tmax, such as rivastigmine patch, could perform a similar efficacy with significantly improved tolerability compared with the oral formulations. In this study, we developed an extended-release microspheres formulation of HupA (called as HAM) with poly(lactide-co-glycolide) (PLGA) as drug carrier. HAM has showed the loading rate as 1.35% (w/w) and yielded 42% with mean particle size at 72.6 μm. In vitro and in vivo pharmacokinetics studies have showed that HAM produced a relatively smooth and continuous drug concentration in 14 days. Furthermore, in vivo pharmacokinetics data have demonstrated that the Cmax was lower and the tmax was considerably later in single intramuscular administration of HAM (1,000 μg/kg) than the counterparts in single intragastric administration of HAT (75 μg/kg/d). Meanwhile, HAM has performed a continuous inhibition to brain AChE activity in normal rats and improvement of memory deficit in Aβ1-40 i.c.v. infused AD rat model for 14 days. The results have suggested that HAM has performed good extended-release properties and good prolonged pharmacological efficacy in vivo in the 2-week period, and could exert a similar efficacy with significantly lowered gastrointestinal side effects as compared with oral formulation.

Preparation and in vitro and in vivo evaluation of HupA PLGA microsphere.

SMND-309 promotes angiogenesis in human umbilical vein endothelial cells through activating erythropoietin receptor/STAT3/VEGF pathways.

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Papers

Antitumor effect and toxicity of Lipusu in rat ovarian cancer xenografts.

Protection of MPTP-induced neuroinflammation and neurodegeneration by rotigotine-loaded microspheres.

Preparation and in vitro and in vivo evaluation of HupA PLGA microsphere.

SMND-309 promotes angiogenesis in human umbilical vein endothelial cells through activating erythropoietin receptor/STAT3/VEGF pathways.