Quality control of residual solvent content in polymeric microparticles.

Organic solvents are the innate part of pharmaceutical industry, playing vital role in the bulk drug substance as well as finished product manufacturing. Even though they are used for various crucial purposes, they still lack therapeutic beneficial effect and can be toxic if present in unacceptable limits in final product. Hence, their concentration must be regulated in the final pharmaceutical formulation. With the major development in the market of polymeric microparticles in past few decades, drug product manufacturers are paying more attention towards the development of new techniques for reducing residual solvent content of microparticles. This article sheds light on the importance of removal of organic volatile impurities from the formulation and its regulatory aspects. It also highlights how residual solvent affects various physicochemical characteristics of polymeric microparticles and suggests certain solutions as per the current state of art for limiting organic solvent content in the final product.

Evaluation of anti-metastatic potential of Cisplatin polymeric nanocarriers on B16F10 melanoma cells.

Nanoparticles are being increasingly used in the field of cancer treatment due to their unique properties and advantages. The aim of the present research work was to prepare and characterize a polymeric albumin nanosystem for Cisplatin and evaluate its in-vitro efficacy against B16F10 melanoma. The developed nanoparticles were almost spherical in shape with a particle size in the range of 150-300 nm, low polydispersity values and about 80% drug entrapment efficiency. Albumin nanocarriers sustained the release of Cisplatin for more than 48 h, suggesting the reduction in dosing schedule for this drug. The results from in-vitro cell line studies indicated the dose dependent cytotoxic potential of drug loaded albumin nanoparticles, their potential to inhibit cell proliferation and induce morphological changes. In addition, these nanoparticles exhibited superiority to Cisplatin in hampering the cell migration. Developed nanoparticles caused cell cycle arrest along with time and concentration dependent cellular uptake in B16F10 cell line. These results signify that the prepared Cisplatin albumin nanoparticles could serve as a promising approach for B16F10 melanoma treatment.

Unraveling the cytotoxic potential of Temozolomide loaded into PLGA nanoparticles.

BACKGROUND: Nanotechnology has received great attention since a decade for the treatment of different varieties of cancer. However, there is a limited data available on the cytotoxic potential of Temozolomide (TMZ) formulations. In the current research work, an attempt has been made to understand the anti-metastatic effect of the drug after loading into PLGA nanoparticles against C6 glioma cells.Nanoparticles were prepared using solvent diffusion method and were characterized for size and morphology. Diffusion of the drug from the nanoparticles was studied by dialysis method. The designed nanoparticles were also assessed for cellular uptake using confocal microscopy and flow cytometry. RESULTS: PLGA nanoparticles caused a sustained release of the drug and showed a higher cellular uptake. The drug formulations also affected the cellular proliferation and motility. CONCLUSION: PLGA coated nanoparticles prolong the activity of the loaded drug while retaining the anti-metastatic activity.

Corrigendum: Formulation and development of transferrin targeted solid lipid nanoparticles for breast cancer therapy.

[This corrects the article DOI: 10.3389/fphar.2020.614290.].

Nanotechnology-based approaches applied to nutraceuticals.

Nutraceuticals and food industries are opening to a tremendously upcoming technology in the field of "Nano science". A new prospect has been defined by nanotechnology by conferring modified properties of nanomaterials and its application in the development of nanoformulations, nutritional supplements and food industry. Nanomaterials reveal exclusive properties because of their small size and high surface/volume ratio; thus, they have a complete application in nutraceuticals and food sector. In the existent review article, we obligate to present a comprehensive outline of the application of nanomaterials in development of advanced nano-based nutraceuticals with enhanced bioavailability, solubility, improved encapsulation efficiency, increased stability, sustained and targeted drug delivery, protection against degradation and microbial contamination and with improved pharmacological activity. It also highlights the importance of nanomaterials as nanosensors/nano-bio sensors for encapsulating peptides, antibodies, enzymes, etc. and in the food packaging industry and its future application. Thus, the review aims to focus on the benefits and new dimensions provided by nanomaterials and nanotechnology in health sectors by improving treatment strategies and quality of life.

Fighting Strategies Against the Novel Coronavirus Pandemic: Impact on Global Economy.

Sudden outbreak of a new pathogen in numbers of pneumonic patients in Wuhan province during December 2019 has threatened the world population within a short period of its occurrence. This respiratory tract-isolated pathogen was initially named as novel coronavirus 2019 (nCoV-2019), but later termed as SARS-CoV-2. The rapid spreading of this infectious disease received the label of pandemic by the World Health Organization within 4 months of its occurrence, which still seeks continuous attention of the researchers to prevent the spread and for cure of the infected patients. The propagation of the disease has been recorded in 215 countries, with more than 25.5 million cases and a death toll of more than 0.85 million. Several measures are taken to control the disease transmission, and researchers are actively engaged in finding suitable therapeutics to effectively control the disease to minimize the mortality and morbidity rates. Several existing potential candidates were explored in the prevention and treatment of worsening condition of COVID-19 patients; however, none of the formulation has been approved for the treatment but used under medical supervision. In this article, a focus has been made to highlight on current epidemiology on the COVID-19 infection, clinical features, diagnosis, and transmission, with special emphasis on treatment measures of the disease at different stages of clinical research and the global economic influence due to this pandemic situation. Progress in the development on vaccine against COVID-19 has also been explored as important measures to immunize people. Moreover, this article is expected to provide information to the researchers, who are constantly combating in the management against this outbreak.

Formulation and Development of Transferrin Targeted Solid Lipid Nanoparticles for Breast Cancer Therapy.

Breast cancer is conventionally treated by surgery, chemotherapy and radiation therapy followed by post operational hormonal therapy. Tamoxifen citrate is a best option to treat breast cancer because its selective estrogen receptor modulation activity. Owing to its antiestrogenic action on breast as well as uterine cells, Tamoxifen citrate shows uterine toxicity. The dose 20 mg per day of Tamoxifen citrate required to show therapeutic effect causes side effects and toxicity to vital organs such as liver, kidney and uterus. In the present study, transferrin-conjugated solid lipid nanoparticles (SLNs) were successfully prepared to enhance the active targeting of tamoxifen citrate in breast cancer. Developed formulations were evaluated for particle size, surface charge, surface morphology and in vitro dissolution studies. Developed formulations exhibited more cytotoxicity as compared to pure Tamoxifen citrate solution in time as well as concentration dependent manner on human breast cancer MCF-7 cells. Further, cell uptake and flow cytometry studies confirmed the qualitative uptake of developed D-SLN and SMD-SLN by human breast cancer MCF-7 cells. Overall, proposed study highlights that transferrin engineered nanocarriers could enhance the therapeutic response of nanomedicines for breast cancer treatment.

Hepatoprotective Ayurvedic plants - a review.

The liver plays vital functions in the maintenance and performance of the body. Most of the metabolic and physiological processes of our body as well as the detoxification of various drugs and xenobiotic chemicals occur in the liver. During this detoxification process, the reactive chemical intermediates damage the liver causing hepatotoxicity. Therefore, the maintenance of a healthy liver is vital to overall health. Unfortunately, the liver is often abused by environmental toxins, poor eating habits, alcohol, and prescription and over-the-counter drug use, which lead to liver diseases like hepatitis, non-alcoholic fatty liver disease, alcoholic liver disease, cirrhosis and hepatocellular carcinoma. The available synthetic drugs to treat liver disorders in this condition also cause further damage to the liver on long-term use. Hence, Ayurvedic plants have become increasingly popular and their use is widespread. Various Ayurvedic formulations are available in market to treat liver disease. Also there is increase in the export of Ayurvedic plants.

Thermosensitive PLA based nanodispersion for targeting brain tumor via intranasal route.

Delivery of drugs to the brain via nasal route has been studied by many researchers. However, low residence time, mucociliary clearance and enzymatically active environment of nasal cavity pose many challenges to successful nasal delivery of drugs. We aim to deliver methotrexate by designing thermosensitive nanodispersion exhibiting enhanced residence time in nasal cavity and bypassing the blood brain barrier (BBB). PLA nanoparticles were developed using solvent evaporation technique. The developed nanoparticles were further dispersed in prepared thermosensitive vehicle of poloxamer 188 and Carbopol 934 to impart the property of increased residence time. The formulated nanoparticles demonstrated no interaction with the simulated nasal fluids (SNF), mucin, serum proteins and erythrocytes which demonstrate the safety of developed formulation for nasal administration. The penetration property of nanoparticles though the nasal mucosa was higher than the pure drug due to low mucociliary clearance. The developed nanoparticles diffused though the membrane pores and rapidly distributed into the brain portions compared to the pure drug. There was detectable and quantifiable amount of drug seen in the brain as demonstrated by in vivo brain distribution studies with considerably low amount of drug deposition in the lungs. The pharmacokinetic parameters demonstrated the enhancement in circulation half life, area under curve (AUC) and Cmax of the drug when administered intranasal in encapsulated form. Thus, the thermosensitive nanodispersions are surely promising delivery systems for delivering anticancer agents though the nasal route for potential treatment of brain tumors.

Etoposide loaded solid lipid nanoparticles for curtailing B16F10 melanoma colonization in lung.

Poor solubility of etoposide and associated poor bioavailability of the drug was circumvented by developing solid lipid nanocarrier system. The objective of the research work was to prepare etoposide loaded solid lipid nanoparticles (SLN) for improved efficacy and therapy of metastasized cancers. Entrapment of drug into nanoparticulate system modifies the pharmacokinetic and biodistribution profile of the drug with improved therapeutic efficacy. Solid lipid nanoparticles of various triglycerides were prepared using hot homogenization technique. Further, the process and formulation parameters viz. homogenization cycle and pressure, type of lipid were optimized. Developed nanoparticles were characterised for particle size, in vitro dissolution studies, DSC thermogram, surface morphology and cytotoxicity assay. Pharmacokinetic and biodistribution study were performed to assess the distribution of the drug in vivo. Modulation of the therapeutic activity of the drug was studied by performing antimetastatic activity on a B16F10 melanoma mouse model. The obtained results exhibited suitability of trimysristin for fabrication of nanoparticles. Characterisation of nanoparticles depicted formation of homogenous, spherical particles entrapping approximately 50% of the drug. The results for the performed MTT assay suggested that the developed nanoparticles exhibited cytotoxicity in a time- and concentration-dependent fashion. These findings concord with the results of the in vitro dissolution profile. Pharmacokinetic parameters demonstrated increase in area under curve (AUC), t1/2 and mean residence time (MRT) for drug in plasma. Further there is enhancement in the ratio of the drug that reaches to the highly perfused organs (upon encapsulation into solid lipid nanoparticles). Generally, cancer cells metastasized through the blood or lymphatic system. Accumulation of the drug in the highly perfused organ suggests suitability of the developed nanoparticles for targeting metastasized tumors. This was proved by the findings of the in vivo B16F10 mouse melanoma model. Improvement in the tumoricidal activity and survival rate of the animals substantiates the application of nanoparticles for improved therapeutic activity of etoposide.