Enhancing pharmaceutical potential and oral bioavailability of Allium cepa nanosuspension in male albino rats using response surface methodology

Objective: To enhance the pharmaceutical potential and oral bioavailability of quercetin contents of Allium cepa peel extract by novel nanosuspension technology. Methods: Nanoprecipitation approach was successfully used for the formulation of nanosuspension. To obtain pharmaceutical-grade nanosuspension with minimum particle size and polydispersity index, sodium lauryl sulphate was selected as a stabilizer. Important formulation parameters were statistically optimized by the response surface methodology approach. The optimized nanosuspension was subjected to stability and in vitro dissolution testing and characterized by scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, and zeta sizer. To evaluate the preeminence of nanosuspension over coarse suspension, comparative bioavailability studies were carried out in male albino rats. The pharmaceutical potential of developed nanosuspension was evaluated by antioxidant, antimicrobial, and toxicity studies. Results: The optimized nanosuspension showed an average particle size of 275.5 nm with a polydispersity index and zeta potential value of 0.415 and -48.8 mV, respectively. Atomic force microscopy revealed that the average particle size of nanosuspension was below 100 nm. The formulated nanosuspension showed better stability under refrigerated conditions. Nanosuspension showed an improved dissolution rate and a 2.14-fold greater plasma concentration of quercetin than coarse suspension. Moreover, the formulated nanosuspension exhibited enhanced antioxidant and antimicrobial potential and was non-toxic. Conclusions: Optimization of nanosuspension effectively improves the pharmaceutical potential and oral bioavailability of Allium cepa extract.

Enhancing pharmaceutical potential and oral bioavailability of Allium cepa nanosuspension in male albino rats using response surface methodology

@# Objective: To enhance the pharmaceutical potential and oral bioavailability of quercetin contents of Allium cepa peel extract by novel nanosuspension technology. Methods: Nanoprecipitation approach was successfully used for the formulation of nanosuspension. To obtain pharmaceutical-grade nanosuspension with minimum particle size and polydispersity index, sodium lauryl sulphate was selected as a stabilizer. Important formulation parameters were statistically optimized by the response surface methodology approach. The optimized nanosuspension was subjected to stability and in vitro dissolution testing and characterized by scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, and zeta sizer. To evaluate the preeminence of nanosuspension over coarse suspension, comparative bioavailability studies were carried out in male albino rats. The pharmaceutical potential of developed nanosuspension was evaluated by antioxidant, antimicrobial, and toxicity studies. Results: The optimized nanosuspension showed an average particle size of 275.5 nm with a polydispersity index and zeta potential value of 0.415 and -48.8 mV, respectively. Atomic force microscopy revealed that the average particle size of nanosuspension was below 100 nm. The formulated nanosuspension showed better stability under refrigerated conditions. Nanosuspension showed an improved dissolution rate and a 2.14-fold greater plasma concentration of quercetin than coarse suspension. Moreover, the formulated nanosuspension exhibited enhanced antioxidant and antimicrobial potential and was non-toxic. Conclusions: Optimization of nanosuspension effectively improves the pharmaceutical potential and oral bioavailability of Allium cepa extract.

Nanosuspension enhances dissolution rate and oral bioavailability of Terminalia arjuna bark extract in vivo and in vitro

Objective: To enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract by formulating its nanosuspension. Methods: Nanoprecipitation approach was used for the formulation of nanosuspension using polysorbate-80 as a stabilizer. The formulated nanosuspension was assessed for particle size, polydispersity index, zeta potential value and for in vitro dissolution study. Oral bioavailability studies were carried out in Wistar male albino rats by administering a single dose (50 mg/kg. b. wt) of the formulated nanosuspension and coarse suspension. The storage stability of the formulated nanosuspension was determined after three months of storage at room temperature and under the refrigerated condition. Mutagenicity assay was carried out to evaluate the toxicity of the formulated nanosuspension using two mutant strains (Salmonella typhimurium TA100 and Salmonella typhimurium TA98). Results: The mean particle size of the formulated nanosuspension was 90.53 nm with polydispersity index and zeta potential values of 0.175 and-15.7 mV, respectively. Terminalia arjuna nanosuspension showed improved dissolution rate and 1.33 fold higher oral bioavailability than its coarse suspension. The formulated nanosuspension also showed better stability under the refrigerated condition and was non-mutagenic against both strains. Conclusions: Our study demonstrates that nanosuspension technology can effectively enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract. Zafar Fatiqa 1 Department of Chemistry, University of Okara, Okara Jahan Nazish 2 Department of Chemistry, University of Agriculture, Faisalabad Khalil-Ur-Rahman 3 Department of Biochemistry, University of Agriculture, Faisalabad Asi Muhammad 4 Food Toxicology Lab, Plant Protection Division, Nuclear Institute for Agriculture and Biology, Faisalabad Zafar Waseeq-Ul-Islam 5 Department of Computer Science, COMSATS University of Information and Technology, Islamabad Pawar SS, Dahifale BR, Nagargoje SP, Shendge RS. Nanosuspension technologies for delivery of drugs. Nanosci Nanotech Res 2017; 4(2): 5966. Kilor V, Sapkal N, Daud A, Humne S, Gupta T. Development of stable nanosuspension loaded oral films of glimepiride with improved bioavailability. Int J Appl Pharm 2017; 9(2): 28-33. He J, Han Y, Xu G, Yin L, Neubi MN, Zhou J, et al. Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement. RSC Adv 2017; 7: 13053-13064. 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Synergistic interactions of polyphenols and their effect on antiradical potential

The aim of the current study was to evaluate interactions among polyphenols from different plants and their effect on antioxidant potential. Different mixtures of plant extracts of Crataegus oxyacantha [C], Elettaria cardamomum [Cr], Terminalia arjuna [T] and Rauvolfia serpentina [R] were prepared and evaluated for total phenolics, flavonoid contents, and antioxidant activity. A correlation was also established between total phenolics, flavonoids and antioxidant activity. Comparative evaluation revealed that phenolics, flavonoids and antioxidant activity were found high in plant extracts mixtures than individual plants. Highest phenolics [580+/-1.12mg GAE/g], flavonoids [67.10+/-0.11mg CE/g] and antioxidant activity [IC[50] 0.109mg/ml] was observed with ratio 1:1:1:2 of plant mixture C, Cr, T, R. A weak linear positive correlation was found between antioxidant activity, total phenolic and flavonoid contents. A negative correlation was observed among IC[50] value, total phenolics and flavonoid contents. Investigation through RP-HPLC revealed the presence of different potent phenolics in plants understudy. More antioxidant potential of extracts in combinations as compared to that of individual plants was clear corroboration of synergism. The ratio [1:1:1:2] of the studied plants in combination, that showed the highest free radical potential, was another expected better pharmacological prospect. This formulation can bring maximum relief against free radical-associated diseases