Studies on in-vitro transcutaneous delivery of losartan potassium, influence of penetration enhancers and barrier membrane

Formulation and in vitro evaluation of losartan potassium (LP) loaded transdermal delivery system (TDS) was investigated for controlled release and improved therapeutic efficacy. TDS (patches) were prepared by varying the composition of Eudragit RL 100 and Eudragit RS 100 (5:0, 4:1, 3:2, 2.5:2.5, 2:3, 1:4 and 0:5). Patches were evaluated for thickness, content uniformity, mechanical properties, moisture uptake and in vitro drug release. Technological parameters for all the formulations were found to be within the limit. In vitro studies showed relatively high permeation of LP (F1- 42.17 ± 1.13 %) from the formulation comprising 4:1 ratio of polymer. Inclusion of capsaicin (55.70 ± 1.55 %) and pluronic F-68 (70.88 ± 1.20 %) to formulation F1 resulted increased permeation of LP across human skin. In conclusion, this study demonstrated the potential of simple transdermal adhesive patch incorporating LP to deliver therapeutically useful dose in-vivo for the treatment of hypertension.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development of Novel Octanoyl Chitosan Nanoparticles for Improved Rifampicin Pulmonary Delivery: Optimization by Factorial Design

A novel hydrophobic chitosan derivative, octanoyl chitosan (OC) with improved organic solubility was synthesized, characterized, and employed for the preparation of rifampicin (Rif) encapsulated nanoparticle formulations for pulmonary delivery. OC was characterized to confirm acyl group substitution and cytotoxicity in A549 epithelial lung cells. OC nanoparticles were produced by the double emulsion solvent evaporation technique without cross-linking and characterized for particle size distribution, morphology, crystallinity, thermal stability, aerosol delivery, and drug release rate. OC was successfully synthesized with substitution degree of 44.05 ± 1.75%, and solubility in a range of organic solvents. Preliminary cytotoxicity studies of OC showed no effect on cell viability over a period of 24 h on A549 cell lines. OC nanoparticles were optimized using a 32full factorial design. An optimized batch of OC nanoparticles, smooth and spherical in morphology, had mean hydrodynamic diameter of 253 ± 19.06 nm (PDI 0.323 ± 0.059) and entrapment efficiency of 64.86 ± 7.73% for rifampicin. Pulmonary deposition studies in a two-stage impinger following aerosolization of nanoparticles from a jet nebulizer gave a fine particle fraction of 43.27 ± 4.24%. In vitro release studies indicated sustained release (73.14 ± 3.17%) of rifampicin from OC nanoparticles over 72 h, with particles demonstrating physical stability over 2 months. In summary, the results confirmed the suitability of the developed systems for pulmonary delivery of drugs with excellent aerosolization properties and sustained-release characteristics. © 2018, American Association of Pharmaceutical Scientists

An Overview of Nanocarrier-Based Adjuvants for Vaccine Delivery

The development of vaccines is one of the most significant medical accomplishments which has helped to eradicate a large number of diseases. It has undergone an evolutionary process from live attenuated pathogen vaccine to killed whole organisms or inactivated toxins (toxoids), each of them having its own advantages and disadvantages. The crucial parameters in vaccination are the generation of memory response and protection against infection, while an important aspect is the effective delivery of antigen in an intelligent manner to evoke a robust immune response. In this regard, nanotechnology is greatly contributing to developing efficient vaccine adjuvants and delivery systems. These can protect the encapsulated antigen from the host’s in-vivo environment and releasing it in a sustained manner to induce a long-lasting immunostimulatory effect. In view of this, the present review article summarizes nanoscale-based adjuvants and delivery vehicles such as viral vectors, virus-like particles and virosomes; non-viral vectors namely nanoemulsions, lipid nanocarriers, biodegradable and non-degradable nanoparticles, calcium phosphate nanoparticles, colloidally stable nanoparticles, proteosomes; and pattern recognition receptors covering c-type lectin receptors and toll-like receptors