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Nanocarrier Technologies for Enhancing the Solubility and Dissolution Rate of Api
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Ashwini Deshpande, Tulshidas S. Patil
In another recent study by Janga and Dudhipala, oral bioavailability of poorly water-soluble drug zaleplon was enhanced by 2.66-fold by implementing Box-Behnken design to develop solid lipid nanoparticles [17].
Antiviral Drugs as Tools for Nanomedicine
Published in Devarajan Thangadurai, Saher Islam, Charles Oluwaseun Adetunji, Viral and Antiviral Nanomaterials, 2022
Polymeric micelles are nanospheres less than 100 nm diameter that were aimed to improve aqueous solubility, intestinal permeability, and disease site targeting of several drug molecules. Different polymeric microspheres formulations are reported as drug-delivery systems for antivirals. Saquinavir-loaded poly (ethylene oxide)-modified poly (epsilon-caprolactone) (PEO-PCL) polymeric nanoparticulate system was developed by Shah and Amiji (2006). This novel formulation aimed for intracellular delivery of SQV at a significantly higher level through the medium of nanoparticles formulation in THP-1 human monocyte/macrophage (Mo/Mac). ARV drug release from poly (DL-lactide-co-glycolide) NPs in BALB/c mice was evaluated by Destache et al. (2010). They administered free ritonavir, lopinavir, and efavirenz (EFV) intraperitoneally and compared with the same drugs’ nanoparticles formulation. Serum-free ARV drug concentrations peaked 4 h post-injection and were eliminated by 72 hours, whereas poly (DL-lactide-co-glycolide) NPs, animals had detectable ritonavir, lopinavir, and EFV concentrations in all tissues for 28 days. ARV nanoparticles treatment of monocyte-derived macrophages demonstrated sustained inhibition of HIV-1 replication (Destache et al. 2010). Tenofovir-loaded chitosan-based nanoparticles showed mucoadhesive properties due to the cationic charge on the chitosan molecule (Meng et al. 2011). Meng et al used the Box-Behnken design to evaluate the effect of formulation variables on the NPs size and drug encapsulation efficiency (EE%). This chitosan-based NP formulation was found to be non-cytotoxic to the vaginal epithelial cell line for 48 hours. The study demonstrated that the percentage of mucoadhesion increased from 6% to 12% as the diameter reduced from 900 nm to 188 nm, respectively (Meng et al. 2011). The study by Neves et al. (2010) demonstrated that polyethylene oxide-coated nanoparticles reduced permeability across monolayers/tissues, while modification of nanosystems with cetyltrimethylammonium bromide (CTAB) enhanced transport. Lamivudine stearate (LAS) was studied by Li et al. (2010). The team also studied the antiviral activity of LAS encompassed in stearic acid-γ-chitosan oligosaccharide (CSO-SA) polymeric micelles. LAS was synthesised with an ester linkage between lamivudine (LA) and stearic acid. CSO-SA/LAS presented low cytotoxicity and high cellular uptake percentage of LAS against HBV-transfected tumour cells (HepG2.2.15) (Li et al. 2010). Chiappetta et al. (2011) studied oral pharmacokinetics of the anti-HIV efavirenz (EFV) encapsulated within polymeric micelles in adult healthy volunteers. The micelles demonstrated consistent results and significantly higher absorption rates and the pharmacokinetic (PK) parameters increased 3-fold higher.
Innovative Delivery Systems for Andrographolide Delivery
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
A. C. Santos, J. A. D. Sequeira, F. Veiga, A. Figueiras, A. J. Ribeiro
A strategy that combines the features of nanocrystals and the direct compression technologies used for the classic production of tablets was developed as a novel solution for the oral delivery of AG (Xu et al., 2017). Here, the central premise was turning liquid nanosuspensions into a dried nanocrystal powder, which might have a better wettability (Merisko-Liversidge et al., 2003) by spray-drying or freeze-drying, and ultimately convert it into a solid dosage form (Van Eerdenbrugh et al., 2008). The authors initially produced AG nanocrystals by homogenization through the optimizing of the formulations variables using Box–Behnken design as a rational experiment design. This was followed by the application of spray-drying to produce an AG nanocrystal-based dry powder. AG nanosuspensions evidenced a particle size of 509.21 nm. TPGS and PVPK30 were chosen as the stabilizing agents, and two types of formulation were produced and compared. The produced AG nanocrystals were analyzed by differential scanning calorimetry and powder X-ray diffraction techniques. It was found that homogenization followed by freeze drying used as the technique for particle reduction did not tamper with the crystal structure of AG proving to be adequate to reduce the crystal to nanosize. Following the production of the nanocrystals, these were mixed with MCC and lactose as matrix formers to form AG nanocrystal-based compressed tablets for oral delivery (Xu et al., 2017). Following a redispersibility study, a mixture of 50% MCC and 50% lactose as matrix formers was selected to prevent the irreversible agglomeration of the AG nanocrystal particles during spray-drying and compression. The reduced particle size of the AG nanocrystals resulted in the increase of surface area. The optimization of the surface wetting was achieved by TPGS and PVPK30, which significantly increased the dissolution rate of AG. Dissolution studies in pure water of AG nanocrystal-based compressed tablets achieved 85.87% of dissolution after 30 minutes compared with 31.15% and 33.37% for the free AG and the physical mixture, respectively. Male Wistar rats received an oral single dose (10 mg/kg) of AG nanocrystal compressed tablets with TPGS as the nanocrystal stabilizer. It was observed that AG nanocrystal-based compressed tablets exhibited a fast tmax of 0.86 h, and a higher Cmax of 299.32 ± 78.54 ng/mL in comparison with the free unprocessed AG, respectively, with a tmax of 1.47 h and Cmax of 77.52 ± 31.73 ng/mL. The analysis of these pharmacokinetic parameters shows evidence that this formulation enhanced the AG solubility, being that the oral bioavailability was 3.09-times higher than for the free unprocessed AG. That finding might be linked to the fact that it attributed to TPGS the inhibition of P-glycoprotein efflux pump, which contributes to the increase of the oral bioavailability of low soluble and permeable drugs, the BCS class II drugs, such as AG (Xu et al., 2017).
Optimization of dropping process of Xuesaitong dropping pills based on quality by design concept and machine vision
Published in Drug Development and Industrial Pharmacy, 2023
Yizhe Hou, Xi Wang, Zhiyong Zhang, Jiaheng Wu, Xiang Cai, Pian Li, Zheng Li, Wenlong Li
According to the previous work of this research group [24], four CPPs were investigated in experiments, which were material ratio (MR, ratio of polyethylene glycol 4000 to NTS), coolant top temperature (CTT), coolant bottom temperature (CBT), and DD. Generally, the PBD combined with response surface methodology is an excellent way to estimate multi-factors. The Box–Behnken design is a kind of response surface design, which is often used to investigate the nonlinear influence of factors, and can effectively estimate the first-order and second-order coefficients [25]. Therefore, the BBD experiment of four factors at three levels (total 27 runs) was applied to investigate the relationships between CPPs and CQAs in this study (the PBD and BBD was run with Design Expert software). The coded and uncoded values of parameters are listed in Table 1. The specific experimental conditions and results of the BBD are listed in Table 2, and the experiments were carried out according to the order in the table. The construction of design space (the design space was run with MATLAB software) should first set the acceptable range and compliance probability of the CQAs according to the production requirements, as shown in Table 3, and then calculate the corresponding operation range of the CPPs according to the requirements. After the development of design space, verification experiments were carried out to verify the reliability of the design space. Each validation experiments were repeated three times.
Solid lipid nanoparticles by Venturi tube: preparation, characterization and optimization by Box–Behnken design
Published in Drug Development and Industrial Pharmacy, 2021
Gilberto García-Salazar, María de la Luz Zambrano-Zaragoza, Eduardo Serrano-Mora, Sandra Olimpia Mendoza-Díaz, Gerardo Leyva-Gomez, David Quintanar-Guerrero
There are two ways to reach the goals of experimental research. The first consists of the variation of one factor at a time while maintaining all others constant. However, this step-by-step method is tedious and does not show the interaction between two or more factors [12]. The second approach uses an experimental design that is efficient for estimating the effects of several variables simultaneously using a factorial approach. A statistical factorial design makes it possible to analyze several variables simultaneously and provides information not generated in classical experimental methods, namely, interactions among variables [13]. The Response Surface Methodology is one approach that can evaluate the relations between the response and independent variables simultaneously [14] while helping to determine the optimum operating conditions to decrease the number of experiments required. The Box-Behnken design in our study allowed us to use fewer experiments than the central composite or three-level full factorial design. The explanation is that this design does not require experiments at the experimental region's vertices to avoid performing procedures under extreme conditions that can make such experiments difficult to conduct adequately [15].
Development of UV–visible spectrophotometric methods for the quantitative and in silico studies for cilazapril optimized by response surface methodology
Published in Drug Development and Industrial Pharmacy, 2021
The criteria to select the statistical design for this study are to examine the relationship between the desired response and the independent variables utilizing second degree polynomial model. Statistical design like response surface methodology (RSM) based on the Box–Behnken design is an edge over classical method by optimizing the various variables critical for the study and evaluating their effect simultaneously. To have the suitable regression equation, the analysis of experimental data was performed by linear, two factor interaction and quadratic models. The statistical data from different source models are given in Table S3 (method A) and Table S4 (method B) (Supplementary). The statistics from source models were compared and the quadratic model for both the methods were chosen based on highest R2 value, high F value, lower standard deviation value, lower p value (<.0001), and minimum PRESS values. Also, results from quadratic model further suggested that the model is accurate in predicting the response. The relation between the predicted response and the independent experimental variables for the quadratic model is shown below: