Destabilization Mechanism of Ionic Surfactant on Curcumin Nanocrystal against Electrolytes.

We have successfully developed curcumin nanosuspension intended for oral delivery. The main purpose is to improve bioavailability through enhancing its solubility. The nanoparticles were stabilized using various stabilizers, including polyvinyl pyrrolidone (PVP), polyvinyl alcohol (PVA), sodium carboxymethylcellulose (Na-CMC), d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), and sodium dodecyl sulfate (SDS). The average diameter of particles, microscopic appearance, and sedimentation of each preparation was observed and compared. Each stabilizer demonstrated a different degree of inhibition of particle aggregation under electrolyte-containing simulated gastrointestinal (GIT) fluid. Non-ionic stabilizers (PVA, PVP, and TPGS) were shown to preserve the nanosuspension stability against electrolytes. In contrast, strong ionic surfactants such as SDS were found to be very sensitive to electrolytes. The results can provide useful information for the formulators to choose the most suitable stabilizers by considering the nature of stabilizers and physiological characteristics of the target site of the drug.

Development of curcumin nanocrystal: physical aspects.

Curcumin, a naturally occuring polyphenolic phytoconstituent, is isolated from the rhizomes of Curcuma longa Linn. (Zingiberaceae). It is water insoluble under acidic or neutral conditions but dissolves in alkaline environment. In neutral or alkaline conditions, curcumin is highly unstable undergoing rapid hydrolytic degradation to feruloyl methane and ferulic acid. Thus, the use of curcumin is limited by its poor aqueous solubility in acidic or neutral conditions and instability in alkaline pH. In the present study, curcumin nanocrystals were prepared using high-pressure homogenization, to improve its solubility. Five different stabilizers [polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), d-α-tocopherol polyethylene glycol 1000 succinate (TPGS), sodium dodecyl sulfate (SDS), carboxymethylcellulose sodium salt] possessing different stabilization mechanism were investigated. The nanoparticles were characterized with regard to size, surface charge, shape and morphology, thermal property, and crystallinity. A short-term stability study was performed storing the differently stabilized nanoparticles at 4°C and room temperature. PVA, PVP, TPGS, and SDS successfully produced curcumin nanoparticle with the particle size in the range of 500-700 nm. PVA, PVP, and TPGS showed similar performance in preserving the curcumin nanosuspension stability. However, PVP is the most efficient polymer to stabilize curcumin nanoparticle. This study illustrates that the developed curcumin nanoparticle held great potential as a possible approach to improve the curcumin solubility then enhancing bioavailability.

Production and characterization of antioxidant apigenin nanocrystals as a novel UV skin protective formulation.

Flavonoids have many positive effects on various cell layers of the skin (e.g. anti-oxidant, anti-allergic and anti-inflammatory effects). However, the limiting factor of the use of flavonoids is their low water solubility. To overcome the poor solubility, apigenin nanosuspensions were prepared using the combination technology (CT), i.e. bead milling and subsequently high pressure homogenization. Distinct reduction in particle size was observed after each bead milling passage resulting in z-average (PCS) of 413 nm and a polydispersity index of 0.202. The LD data showed a similar pattern of particle size reduction reaching a diameter 99% (d(v)99%) of 0.515 µm. The antioxidant capacity of apigenin nanocrystals were almost doubled compared to the original coarse suspension. The developed smartCrystals can be easily incorporated into gels, which makes apigenin nanocrystals available for dermal application as efficient antioxidant.

Present status of nanoparticle research for treatment of tuberculosis.

Nanotechnology has offered enormous improvement in field of therapeutics by means of designing of drug delivery systems and opened the possibility of controlling infections at the molecular level. Nanocarriers can cross biological barriers and are able to target cellular reservoirs of Mycobacterium tuberculosis (M. tuberculosis). Nanoparticle-based systems have significant potential for treatment and prevention of tuberculosis (TB). A variety of nanocarriers have been widely evaluated as potential drug delivery systems for various administration routes. Targeting the drugs to certain physiological sites such as the lymph nodes has emerged as a promising strategy in treating TB with improved drug bioavailability and reduction of the dosing frequency. Nanotechnology based rational targeting may improve therapeutic success by limiting adverse drug effects and requiring less frequent administration regimes, ultimately resulting in more patients compliance and thus attain higher adherence levels. The development of nanoparticle based aerosol vaccine is undergoing which could serve as new platform for immunization. Present article compiles the general physiological aspects of the infection along with the relevance nanocarriers used in prevention of tuberculosis.

Production and characterization of Hesperetin nanosuspensions for dermal delivery.

Nanosuspensions of Hesperetin were produced using four different stabilizers, Poloxamer 188, Inutec SP1, Tween 80 and Plantacare 2000, possessing different mechanisms of stabilisation. The nanosuspensions were characterized with regard to size (photon correlation spectroscopy (PCS), laser diffractometry (LD)) and charge (zeta potential measurements). A nanocrystal PCS size of about 300 nm was obtained after 30 homogenization cycles at 1500 bar with the stabilizers Poloxamer, Inutec and Plantacare. Tween was slightly less efficient to preserve the nanocrystal size directly after production (347 nm). The short-term stability was assessed by storage of the nanosuspensions at 4 degrees C, room temperature and 40 degrees C. As predicted from the zeta potential measurements, Inutec and Plantacare stabilized nanosuspensions were stable with no change in PCS diameter and LD diameter 99%. Slight increases in size were found for the Poloxamer and the Tween stabilized nanosuspensions, which is not considered to impair their use in dermal formulations.