Pharmaceutical Nanotechnology - Volume 7, Issue 1, 2019
Volume 7, Issue 1, 2019
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Drug Combinations in Breast Cancer Therapy
Authors: Funmilola A. Fisusi and Emmanuel O. AkalaBreast cancer therapy involves a multidisciplinary approach comprising surgery, radiotherapy, neoadjuvant and adjuvant therapy. Effective therapy of breast cancer requires maximum therapeutic efficacy, with minimal undesirable effects to ensure a good quality of life for patients. The carefully selected combination of therapeutic interventions provides patients with the opportunity to derive maximum benefit from therapy while minimizing or eliminating recurrence, resistance and toxic effects, as well as ensuring that patients have a good quality of life. This review discusses therapeutic options for breast cancer treatments and various combinations that had been previously exploited. The review will also give an insight into the potential application of the nanotechnology platform for codelivery of therapeutics in breast cancer therapy.
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Novel Drug Delivery Strategies for the Treatment of Onychomycosis
Authors: Rupinder K. Dhamoon, Harvinder Popli and Madhu GuptaOnychomycosis accounts for 50% of all nail disease cases and is commonly caused by dermatophytes. It was primarily considered a cosmetic problem but has been garnering attention lately due to its persistent nature and difficult treatment with relapses. With prolonged treatment duration and high cost involved in treating onychomycosis, several attempts have been made in overcoming the rigid nail barrier. The conventional treatment of onychomycosis involves oral and topical therapy. The oral antifungal agents though quite effective, are hepato-toxic and cause drug-drug interactions. Topical therapy is more patient compliant being devoid of such adverse effects but it suffers from another setback of improper nail penetration. Amorolfine and ciclopirox nail lacquers are popular market products. Since decades, efforts have been made to enhance topical delivery for efficiently treating onychomycosis. Mechanical, physical and chemical methods have been employed. Despite all the attempts made, the nail delivery issues are far from being solved. Recently, the focus has shifted to novel drug delivery systems like nanoparticles, microemulsions, polymeric films and nail lacquers for enhanced drug permeation and localized therapy. The research around the world is exploring their potential as effective treatment options. This review intends to further explore the novel delivery strategies to treat a persistent fungal infection like onychomycosis.
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Enhanced Water Dispersibility of Curcumin Encapsulated in Alginate-Polysorbate 80 Nano Particles and Bioavailability in Healthy Human Volunteers
Background: The turmeric (Curcuma longa) plant, a perennial herb of the ginger family, is an agronomic crop in the south and southeast tropical Asia. Turmeric an Indian yellow gold and universal spice is described in Ayurveda, an ancient treatise on longevity and quality life for the treatment of various inflammatory disorders. The oral bioavailability of curcumin is low due to poor aqueous solubility, alkaline instability and speedy elimination. Objective: The present study is designed to prepare alginate polysorbate 80 nanoparticles to enhance aqueous solubility/dispersibility, hence bioavailability. Method: Curcumin-loaded alginate - polysorbate 80 nanoparticles were prepared by ionotropic gelation technique. Results: The optimized nano particles exhibited higher encapsulation efficiency (95%), particle size of 383 nm and Zeta potential of +200 mV. Formulations exhibited very low dissolution in Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF), but the major portion released in SCF which is attributed to the digestibility of alginate in Simulated Colonic Fluid (SCF) under the influence of colonic micro flora. FTIR and DSC observations revealed the successful entrapment of curcumin in alginate polysorbate-80 nanoparticles. The nanoparticles were more spherical, discrete and homogeneous. In healthy human volunteers, the oral bioavailability (AUC) of curcumin increased 5-fold after the consumption of curcumin nanosuspension compared to curcumin suspension. Maximum plasma concentration Cmax- 636 ± 122 ng/ml was observed at tmax- 2h for nanosuspension, whereas Cmax-87.7 ± 17.9ng/ml at tmax- 4h for suspension. Conclusion: Curcumin-loaded alginate - polysorbate 80 nanoparticles prepared by ionotropic gelation method, successfully entrapped curcumin. Both curcumin suspension and curcumin nanosuspension were safe and well tolerated and may thus be useful in the prevention or treatment of various inflammatory diseases of mankind.
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Unusual Enthalpy Driven Self Assembly at Room Temperature with Chitosan Amphiphiles
Authors: Uchechukwu Odunze, Fionn O'Brien, Lisa Godfrey, Andreas Schätzlein and Ijeoma UchegbuBackground: GCPQ (N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl- 6-O-glycolchitosan) is a self-assembling polymer being investigated as a pharmaceutical nano-carrier. GCPQ nanoparticles shuttle drugs across biological barriers, improving drug performance. The exact chemistry of GCPQ is varied by the relative proportion of hydrophobic (N-palmitoyl) and hydrophilic (quaternary ammonium) groups and molecular weight. Objective: We hypothesised that the thermodynamics of self-assembly is controlled by the polymer molecular weight and hydrophobicity. Method: The thermodynamics of self-assembly was investigated using isothermal calorimetry. Results: GCPQs (Mw = 8-15 kDa) formed micellar aggregates at critical micellar concentrations of 1-2.4 μM at 25°C and micellisation was unusually enthalpy driven. There was a positive correlation between ΔHmic and mole% quaternary groups (Q): ΔHmic = 3.8 Q- 159 (r2 = 0.93) and a negative correlation between ΔHmic and molecular weight (Mw): ΔHmic = -13.5 Mw-26.3 (r2 = 0.99). Conclusion: These findings provide insights into the positive drivers of stable selfassemblies, namely hydrophobicity and molecular weight, as both hydrophobicity and molecular weight are associated with an increased enthalpy contribution to micellisation.
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Preparation, Optimization and In vitro Evaluation of Glipizide Nanoparticles Integrated with Eudragit RS-100
Authors: P. Saharan, K. Bahmani and S.P. SaharanBackground: Solubility is an important criterion for drug efficacy, independent of the route of administration. It also poses a major challenge for pharmaceutical industries, which are developing new pharmaceutical products, since 40% of the active substances being identified are either insoluble or poorly soluble in aqueous media. Objective: The objective of this study was to develop nanoformulation of glipizide drugloaded nanoparticles providing controlled release formulation. Method: Nanoparticles were prepared by the solvent evaporation method. Eudragit RS100, a nonbiodegradable polymer with varying ratios was used for making the formulation. The effect of key formulation variables on the particle size and entrapment efficiency and drug loading of nanoparticles were studied by using factorial design. Results: DSC thermograms indicate that glipizide was dispersed in an amorphous state in the polymer. TEM study indicates that the nanoparticles were in spherical shape. The mean diameter was dependent on the presence of the amount of Eudragit RS100 and viscosity of the organic phase. The in vitro study showed that the cumulative drug release was from 69.52-81.44 % in 10 hrs at pH 6.8 in phosphate buffer respectively. Conclusion: The developed NPs could reduce dose frequency, decrease side effects, and improve patient compliance. Using factorial design, maximum entrapment efficiency with minimum particle size could be achieved with a few experiments.
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