The formulations were designed by 32 full-factorial designs using eudragit polymers (S100 and L100) and phosphatidylcholine as dependent variables giving relevant results compared to the conventional product.
There are several vibrational peaks of docetaxel trihydrate were observed in FTIR. The NH stretching of alkanes, C-O stretching vibration, N-H plane bonding vibrations, and C = O stretching were observed at 3432 cm− 1, 1782 cm− 1, 1635 cm− 1, and 720 cm− 1. With the drug and polymers mixture peaks were observed at 3375 cm− 1, 1772.61 cm− 1, 1684.85 cm− 1, and 707.89 cm− 1 [Zhuang et al. 2020]. The two-graph of stretching vibrational peaks were matched each other showing that the drug sample used is pure and stable and there are no such interactions were found with drug and Polymers. The DSC thermogram peak of the drug and polymers were found in the range of 115.64 °C. The two graphs of the thermogram were matched with each other and conclude that there is no such interaction found between the drug and polymers.
pH-dependent polymer gated mesoporous silica-loaded docetaxel trihydrate nanoparticles had a narrow size distribution in addition to a significant difference in the distribution between pH-dependent polymer gated mesoporous- silica nanoparticles of docetaxel trihydrate and drug-free pH-dependent polymer gated mesoporous silica loaded docetaxel trihydrate nanoparticles was observed.
The SEM of nanoparticles have smooth with a uniform spherical shape and it also approved the particle size found in the particle size analysis.
The poor encapsulation efficiency of mesoporous silica-loaded docetaxel nanoparticlesis due to low solubility and it has been examined that nanoparticles are increased drug encapsulation efficiency and reduce drug leakage as well as prolong residence and accumulation of drugs at target sites. The drug loading efficiency (%) was enhanced significantly (p < 0.05) as the ratio of Eudragit S100 and L100 and phosphatidylcholine were increased.
The zeta potential range of the nanoparticles is within the range of ± 30 mv, it shows less coalescence and stable nanoparticles due to electrostatic repulsion between particles. The significance of the zeta potential value indicates the stability of the nanoparticles with less coalescence of formulated mesoporous silica-loaded docetaxel trihydrate nanoparticles.
The in-vitro dissolution summary of mesoporous silica loaded docetaxel trihydrate has significant (p < 0.05) enhancement due to the large surface area leading to small particle sizes and polymers (Eudragit S100 and L100) as well as surfactant played an important role in the release rate. This evidence shows that the potential release of mesoporous silica-loaded docetaxel trihydrate indicates the enhancement of therapeutic efficacy through the predictable release of docetaxel trihydrate at the target site. The release pattern of mesoporous silica loaded docetaxel trihydrate followed zero-order kinetics and also followed the Korsmeyer Peppas model indicated from the highest R2 value and n exponent.
The RSM study using design expert software helps to determine individual main factors and interaction factors using the quadratic equation. The ANOVA result clearly states that both the factors such as the ratio of eudragit S100 and L100 and phosphatidylcholine had a significant value (p < 0.05) effect on entrapment efficiency (%), drug release at 6 hours (%), drug release at 10 hours (%).Results shows that non-linearity decreased the entrapment efficiency with increase independent variables of phosphatidylcholine and entrapment efficiency linearly increase with the ration of eudragit S100 and L100 increase, where A mainly increase from − 1 to + 1 level. From the response surface plot, entrapment efficiency was more dependent on the ratio of eudragit S100 and L100 (A) compared to phosphatidylcholine. The results of the response surface plot of drug release showed that greater curvature toward the ratio of eudragit s100 and L100 (A) and flattering of the curve toward phosphatidylcholine as both independent variables impact the release rate.
There is no significant change of clarity and physical appearance was observed by the stability study. The centrifuge test also showed that the formulation had good physical stability. The good stability might be due to low particle size and effect of tween 20. No degradation of docetaxel trihydrate in optimized formulation was also observed.
In vivo studies shown, Cmax quantity of docetaxel significantly increased when using nanosuspension (Formulation) compared with docetaxel microsuspension and arise in relative bioavailability to the dose was determined to be 3 times. The bioavailability study of rats showed that docetaxel's bioavailability was higher for the nanosuspension formulation.