Current Nanomedicine - Volume 7, Issue 2, 2017

Background: In the current pharmaceutical industry, overcoming drug insolubility is a daunting formulation challenge. The most active drugs (with receptor affinity and specificity and low toxicity) are not necessarily the most druggable, lacking high solubility, stability, permeability or absorption. Since insoluble drug particles show poor bioavailability, one of the solutions to this problem is to aid dissolution rate (kinetic) and solubility (thermodynamic) by nanosizing the drug. Thus, during the past few decades, several strategies based on nanotechnology have been adopted to overcome these problems, which increase production costs and require administration of large doses resulting in higher cost/dose ratios. This review discusses techniques to improve bioavailability and solubility through nanosuspensions, nanoparticles (NPs) as well as using various nanocarriers. Methods: Bibliographic databases were screened for peer-reviewed research literature of recent origin. The papers were selected based on the relevance to nanotechnological methods for improving drug solubility. Results: Synthesis of metal-based drug encapsulant or a drug conveyor constituting a metallo- drug can affect the drug release potential and the rate of drug release. Carrier-free nanocrystal colloidal delivery systems are found to efficiently solubilize drugs. Furthermore, solid dispersions which are comprised of two components where a drug crystal (diameter D 50% < 20 μm) along with a carrier/disintegrant have been successfully employed. In the area of self-emulsifying hydrophilic and hydrophobic drugs, micelles, liposomes, selfdispersing tablets and emulsions as well as solid lipid NPs are good candidates for efficiently transporting drugs. In addition, drug complexes with cyclodextrins, calixarenes, cucurbiturils and dendrimers have also led to better solubility and bioavailability. Conclusion: These approaches present significant improvements to the solubility and bioavailability of existing drugs and future discoveries.

Nanotechnology is an advancing field of biomedical science especially in drug delivery system. Nanoceria a part of nanotechnology will appear as an innovative drug delivery carrier in various therapies. The unique ability of nanoceria to switch its oxidation state between +3 and +4 makes it a potent therapeutic option for many diseases associated with oxidative stress, inflammation and also a potent drug delivery agent. Description: In this review article, we focus the main drug delivery mechanisms (autoregeneration and radical scavenger) of nanoceria and its synthesis, characterization, toxicity; application with respect to reactive oxygen species (ROS) mediated disorders.

Background: We created highly effective ointment on the basis of nanoparticles of silver and zinc. The ointment contains active nanoingredients that optimize the healing process. The ointment creates an optimal microenvironment reparative and has antiinflammatory properties. The drug has a high adsorption capacity; it does not have a local anti-irritant and allergic effects. Methods: Silver nanoparticles were prepared by reduction of silver nitrate (AgNO3) with sodium borohydride (NaBH4) in an aqueous medium in the presence of quaternary ammonium compounds (QAC). In our research, a nanoparticle ZnO was synthesized by the sol-gel method. The experiment on the study of the effect of the developed pharmaceutical hydrophilic ointment compositions on burn healing process behaviour was conducted on Wistar rats aged 6 months, weighing up to 250 grams in accordance with international requirements Guide for the Care And Use of Laboratory Animals and the Russian legislation. Results: As a result of the research, we obtained new pharmaceutical hydrophilic ointment compositions with different contents of active components, including nanoscale elements of silver and zinc oxide, which led to a complete recovery of animals in 16-18 days, 6-day faster than conventional treatments of thermal damage to the skin. Conclusion: The studies showed that the ointment composition has good regenerating, antioxidant and wound healing properties due to active proliferation of epithelial tissue in the wound defect area and complete integumentary structures regeneration. Such effect is ensured by the additional components of the ointment, such as glycerin and methyl cellulose, promoting the penetration of active components into the deep panniculus, ensuring the optimal therapeutic effect.

Aim: Sulphasalazine (SSZ), an anti-inflammatory drug, has been widely used as a second line agent for Rheumatoid Arthritis. In this study Nanoprecipitation technique and Ionic gelation techniques were selected for the preparation of Sulphasalazine nanoparticles. Eudragit S100 and Ethyl Cellulose polymers were selected for nanoprecipitation technique and chitosan was chosen as a polymer for inotropic gelation method. A comparative study was performed. Methods: Sulphasalazine loaded Eudragit S100 and Ethyl Cellulose nanoparticles were prepared in five ratios varying the concentration of drug and polymer. Sulphasalazine loaded Chitosan- Tripolyphosphate nanoparticles were prepared by Ionic gelation technique in six ratios by varying the concentration of tripolyphophate solution as well as the concentration of the drug. Results: In nanoprecipitation technique, Out of the five formulations of EC and five formulations of Eudragit, F3 formulation of EC showed promising results with mean particle diameter of 165.3 nm and zeta potential of -47.7 mV with cumulative drug release of 97.89% in 12 h. In Ionic gelation method, out of six formulations, F6 formulation with 0.5% TPP and 4.687 mg/ml drug was considered as the best formulation because of its good stability(-43.8mV) and mean particle diameter (147.9 nm) which produced a sustained drug release of 97.92% in 12 h. Conclusion: On comparing the best formulations of both the techniques, nanoprecipitation was found to be the best technique because of its mean particlediameter (165.4 nm), greater stability (-47.7 mV) and higher drug entrapment efficiency (89.29%).

Objective: Self-microemulsifying drug delivery system (SMEDDS) of aceclofenac was developed to alleviate poor solubility and bioavailability issues. Methods: The selection of components (oil, surfactant and co-surfactant) was based on saturated solubility studies and self emulsification ability. Pseudoternary phase diagrams were constructed to identify the self-emulsifying region. Isopropyl Myristate (IPM) was selected as oil phase; Cremophore as surfactant and Transcutol as co-surfactant (S/CoS mix) (in ratio of 1:1) respectively as optimized components for the SMEDDS formulation. The formulated liquid SMEDDS was evaluated for its self-emulsification time, phase separation, viscosity, cloud point and droplet size analysis. The liquid SMEDDS were converted to Solid SMEDDS by adsorption on solid carrier (Neusilin US2). Solid SMEDDS were further characterized for SEM, XRD, FTIR studies and evaluated for drug content, micrometric properties. Further Solid SMEDDS were compressed into tablet dosage form. Results: In vitro drug release of liquid and Solid SMEDDS, optimized tablet batch was carried out in buffer (pH 7.4) at 37oC. The optimized formulation showed almost 100% drug release in 30 min and it was significantly higher than that of pure drug. Conclusion: The study indicated the significance of aceclofenac SMEDDS as prospective carrier with enhanced dissolution characteristics for oral administration.

Objective: The objective of this study is to screen factors affecting Albendazole nanocrystals. Method: The albendazole nanocrystals were fabricated by antisolvent precipitation followed by spray drying technique. A Plackett and Burman screening design methodology was employed to evaluate the effects of the process and formulation parameters on the % yield and dissolution efficiency. Results: The % yield varied from 48.16 to 66.52% and the dissolution efficiency varied from 67.80 to 78.12. Considering the statistical analysis of the results, it appeared that the aspiration and concentration of drug solution in organic phase were the most important factors affecting the % yield of formulation. The stirring speed and concentration of polymer solution in aqueous phase showed significant effect on dissolution efficiency. TEM study showed nano sized particles. Conclusion: This study revealed the potential of Plackett and Burman design to screen the process and formulation variables affecting properties of albendazole nanocrystals.