Current Nanomedicine - Volume 9, Issue 3, 2019

Soluplus® is a commercially available graft amphipathic copolymer consisting of polyvinyl caprolactam, polyvinyl acetate, and polyethyleneglycol (13% PEG 6000/57% vinyl caprolactam/30% vinyl acetate). Among the various applications of this solubilizer excipient, produced by BASF, such as the production of amorphous solid dispersions of insoluble drugs, Soluplus® has shown to be able to form nano-sized micelles in water or other aqueous solutions, characterized by a very small diameter and an exceptionally narrow size distribution. These formulations allow to improve the solubility and physical stability in aqueous media of poorly soluble drugs. This review summarizes the recent data from literature on the methods of production and characterization of drugloaded nanomicelles based on Soluplus®, highlighting the potential fields of therapeutic application.

Crossing the blood-brain barrier (BBB) and treating brain disorders by delivering therapeutic agents to specific regions of the brain is a challenge. The BBB, naturally evolved, protective physiological barrier acts as a selective permeable membrane in such a way that it allows only nonionic molecules and molecules of low molecular weight to pass through. Treating brain tumor has become a great challenge as the drug molecules of larger size are not able to cross the BBB and reach the target site. The incompetence of techniques for brain-specific delivery of therapeutic molecules has led researchers to increasingly explore the diagnosis and treatment of disorders incurable with present techniques. This article is to discuss the various techniques or methods to deliver drugs to the brain crossing the BBB.

Background: Nanoparticles have considerably been studied for biomedical applications which include biosensing, bioimaging diagnostics, etc. but the effect of shape and size on the nanoparticles has received little attention. The execution of nanoparticles is affected by various factors such as size, shape, surface charge, etc. Objective: In this manuscript, the effects of nanoparticles size and shape on cellular uptake, biodistribution, and half-life of nanoparticles are discussed. The shape of nanoparticles affects the biodistribution, cellular uptake, adhesion strength, half-life circulation, and drug release kinetics and drug clearance. Methods and Results: The shape of the particles enhances the distribution ratio. Particles with a different shape such as spherical shape particles, improve oral drug bioavailability. Rod-like structure of particles showed more specific uptake and less nonspecific uptake in cells related to sphere particles. The size of the particles also affects the binding properties to the receptor and the enthalpic and entropic properties to control the adhesive strength in nanoparticles. Maximum in vitro cellular uptake showed a 10-60nm size range. Nanoparticles that are more than 100nm in size have the ability to penetrate through leaky vasculature into tumors. The size of the nanoparticles affects the biological fate and the large size particles are accumulated in the liver and spleen. Conclusion: The present manuscript specifically deals with the nanocarrier formulation such as cubosomes and hexasomes. The nanoparticles shape has an impact on hydrodynamics significantly and interfaces of vascular targeting. Due to the small particle size of the cubosomes nanoparticles, the cubic phase is more appropriate for the controlled release drug delivery system. It can be concluded from the findings of the literature survey that the size and shape of nanocarriers have a significant effect on pharmaceutical and biomedical adaptation.

Background: The use of natural actives for cosmeceutical benefits has recently gained high popularity due to their low side effects, natural origin and safety. The fruits of Rosehip, a wild shrub native to Europe, Northwest Africa, and Western Asia have been used in traditional medicines since ancient times. Seeds of Rosehip are known to contain more than 50% of polyunsaturated fatty acids. Inherently, this class of phytoconstituents has been reported to exhibit anti-aging potential. Objective: The objective of the present study was to explore and establish the photoprotective potential of Rosehip Seed Oil (RSO) obtained from Rosa rubigenosa and develop a QbD-based topical nanoformulation. Methods: The photo-protective potential of Rosehip Seed Oil was evaluated through various in-vitro tests and biochemical assays. The o/w nanoemulsion (NE) of the oil was prepared by the ultrasonication method following Central Composite Design (CCD) to find the best possible formulation conditions. Nanoemulsion was further formulated into a topical gel and evaluated for its semisolid attributes. Results: The antioxidant property of Rosehip Seed Oil assessed by estimating DPPH free radical scavenging activity revealed that 45μg/ml of oil was equivalent to 8μg/ml of α- tocopherol (standard). The total phenolic content of the oil was estimated to be 5.81μg/ml. IC50 values for anti-collagenase, anti-elastase and anti-hyaluronidase activities were determined and found to be 7.34mg/ml, 42.3mg/ml and 36.34mg/ml, respectively. The particle size, PDI, zeta potential, viscosity and pH of the optimized batch (R2) were found to be 82.73nm, 0.214, -23.0 mV, 6.65cp and 6.94, respectively. The cumulative release of the drug from the nanoemulsion gel was estimated for 7 hrs and found to be 72.34%. Conclusion: Results of all the in vitro studies performed led to the conclusion that Rosehip oil possesses very good antioxidant, anti-inflammatory and photo-protective properties and a nanoformulation of this plant seed oil has the potential to help in assuaging the detrimental effects of UV rays like photoaging.

Background: Treating the disease like diabetes is essential due to its wide range of spreading and heredity issues. Glipizide is the commonly used drug for the treatment of diabetes. Glipizide loaded sustained release nanoparticles have been developed to avoid repeated dosing. Objective: The study aimed to develop glipizide-loaded sustained release nanoparticles and characterize them for different studies. Methods: The aim of the present study was to develop glipizide-loaded sustained release nanoparticles using different polymers by the solvent evaporation method. The polymers; Eudragit (RS 100) in combination with Polycaprolactone (PCL) were used to encapsulate glipizide. Optimization of all parameters was performed as per Design Expert software by utilizing a 32 full factorial design. The developed nanoparticles were characterized using Fourier transformed infrared spectroscopy, X-ray diffraction, scanning electron microscopy and in-vitro drug release study. Results: FE-SEM showed that the surface morphology of nanoparticles was smooth and spherical as well as in an oval shape. FTIR shows there is no interaction between polymers and drug. XRD results showed that the crystallinity of pure glipizide reduced from 89.5 to 56.7% when converted into sustained release nanoparticles formulation. Sustained drug release over the period of 12 h was observed due to well encapsulation of glipizide by the polymers. Conclusion: Glipizide loaded nanoparticles were developed with good encapsulation efficiency using a combination of two different biocompatible polymers. The drug release behavior showed that they can be used to develop the sustained release formulation to reduce the side effect caused by over drug uptake as compared to the conventional formulation.

Background: Currently, cancer is rising as one of the dominant causes of human deaths worldwide. The application of nano-carriers may help to treat cancer through the delivery of anticancer drugs inside the tumor cells. Objective: The foremost objective behind this research was to formulate chondroitin sulfate tailored cellulose acetate phthalate (CSAC) core shield nanoparticles (NPs) containing 5-Fluorouracil (5-FU) as an anticancer drug. Methods: The FTIR and 1H-NMR spectroscopic methods were used to analyze and characterize the formulation of CSAC copolymer. NPs were typified by Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), Atomic Force Microscopy (AFM), Entrapment efficiency and in-vitro drug release. Results: CSAC NPs were found to exhibit moderate release (95.59±0.15% in 34hrs) than CAP NPs (78.97±0.08% in 8 hours). In the course of cytotoxicity examination in A549 cancer cell line, the results revealed that these 5-FU loaded CSAC NPs showed an immense cytotoxic potentiality. Moreover, CSAC NPs exhibit least hemolytic activity when compared with CAP NPs and plain 5-FU. Conclusion: Conclusively, it was found that the CSAC NPs is an efficient carrier system for the better release of 5-FU in lung cancer.