Nanosuspension

Throughout the last 20 years, several trendy technologies are established within the pharmaceutical analysis and development space. The automation of the drug drug discovery method by technologies like high output screening, combinatorial chemistry and computer aided drug design is resulting in a huge range of drug candidates possessing a very good efficacy. Unfortunately, several of drug candidates are a unit exhibiting poor liquid solubility. The use of drug nanocrystal is an universal formulation approach to extend the therapeutic performance of those medication in any route of administration. Drug nanocrystals are crystals with a size range in the nanometer range, meaning that they are nanoparticles with a crystalline character. This review describes the chemistry properties of drug nanocrystals, production method and potential clinical advantages. Poorly soluble medication are usually difficult drawback in drug formulation. Reducing the particle size of a drug to a nono-scale leads to an increased in surface area-to-volume ratio, increased dissolution velocity and improved in vivo performance of poorly soluble drugs.

The purpose of this research work was to formulate fast dissolving film of cefpodoxime proxetil for oral delivery in order to improve oral bioavailability of drug with poor solubility. Cefpodoxime proxetil (CP) is the drug candidate belonging to BCS class IV with poor solubility and poor permeability is and limited oral bioavailability, an orally administered, extended spectrum, semi-synthetic β- lactum antibiotic of cephalosporin class. To improve oral bioavailability, cefpodoxime proxetil nanosuspension was prepared using solvent-antisolvent precipitation technique. Nanosuspension was characterized on the basis of drug concentration in organic phase, temperature, solvent-antisolvent ratio and the time period of stirring on the particle size systematically. Particle size and zeta potential of nanosuspension was observed at 755.6nm and −22.6mV, respectively. Solvent casting method be used in the formation of film, utilizing HPMC E50 as film former, PEG 400 as plasticizer and tween 80 as surfactant. The optimized fast dissolving film formulation F1 showed uniformity of weight (0.091mg), folding endurance (149) drug content uniformity (99.5%), surface pH (6.8) disintegration time (32 seconds in 6.8 PB) and in- vitro drug release 94.2% in 7 min. So, it is concluded from comparison studies between fast dissolving film (FDF) containing pure drug and nanosuspension, fast dissolving film containing cefpodoxime proxetil nanosuspension gives faster and high drug release.

In this present work quercetin nanosuspension (QNS) has been formulated and investigated its anti-tumor activity against Dalton’s lymphoma cells (DLA) in an in vitro model.  Since quercetin is insoluble in water, it has been formulated into nanosuspension in order to improve the solubility as well as dissolution rate of the drug. Quercetin nanosuspension (QNS) was formulated using homogenization method followed by lyophilization process. The QNS was subjected to particle size, zeta-potential, FTIR, solubility study, in-vitro dissolution study and stability study. Further QNS was subjected to anti-oxidant study and anti-tumor study using Dalton’s lymphoma cells. The results showed that Particle size of the QNS was found to be within the range of ~160-200nm. The zeta potential values of QNS were obtained as (3.69mV). Solubility of QNS was found to be 15.41±0.6683µg/ml. QNS could increase the dissolution rate as well as the saturation solubility. QNS showed significant antioxidant activity compared with that of standard ascorbic acid. QNS exhibited dose-dependent anti-tumor activity with DLA cells. This study concluded that formulated QNS exhibited potent antioxidant activity as well as anti-tumor activity.

In this present work Erythromycin stearate nanosuspension has been formulated. Since Erythromycin stearate is insoluble in water, it has been formulated as nanosuspension to improve bioavailability of the drug. The formulation was carried out using High Pressure Homogenization method using different variables like drug-surfactants ratio, stirring speed and rotation time, to optimize the final formulation while keeping the quantities of active ingredient constant. An optimized final formulation was prepared by using drug, poloxamer 188 and tween20 in 1:2:2 ratios with stirring speed of 25000 rpm for 25 minutes using High Pressure Homogenizer (Polytron PT 1600E) followed by lyophilisation. The optimized final formulation was subjected to in-vitro parameters such as compatibility, drug content, particle size analysis, zeta-potential, SEM, in-vitro release profile. All the in vitro evaluation parameters complied the limits. Stability studies were also conducted as per ICH guidelines and from the result it may be concluded that the optimized formulation is stable. Finally, it is concluded that the drug is compatible and stable with the excipients, hence Erythromycin stearate can be formulated as nanosuspension by this method. Key words: Erythromycin stearate, Poloxamer 188, Nanosuspension, Zeta potential, DSC, SEM.    

At current 40% of the drugs were poorly soluble and were also called as “brick dust”. And the drugs which were belonging to the BCS CLASS II & IV were most eligible for this Nanosuspension technology. Here by using different methods we are reducing the particle size so the surface area will be increases ultimately it leads to increase in the bio availability. This instance was observed mostly in the case of anti-cancer drugs. Paclitaxel with 25% of Human Serum Albumin (HSA) showed very good results in terms of drug content, particle size, zeta potential and %CDR. Key words: Nanosuspension, Paclitaxel, Human Serum Albumin (HSA), High pressure homogenization.