Development and Characterization of Venetoclax Nanocrystals for Oral Bioavailability Enhancement

Background: Paclitaxel and spirulina when administered as nanoparticles, are potentially useful. Methods: Nanoformualtions of Paclitaxel and Spirulina for gastric cancer were formulated and optimized with Central composite rotatable design (CCRD) using Response surface methodology (RSM). Results: The significant findings were the optimal formulation of polymer concentration 48 mg, surfactant concentration 45% and stirring time of 60 min gave rise to the EE of (98.12 ± 1.3)%, DL of (15.61 ± 1.9)%, mean diameter of (198 ± 4.7) nm. The release of paclitaxel and spirulina from the nanoparticle matrix at pH 6.2 was almost 45% and 80% in 5 h and 120 h, respectively. The oral bioavailability for the paclitaxel spirulina nanoparticles developed is 24.0% at 10 mg/kg paclitaxel dose, which is 10 times of that for oral pure paclitaxel. The results suggest that RSM-CCRD could efficiently be applied for the modeling of nanoparticles. The paclitaxel and spirulina release rate in the tumor cells may be higher than in normal cells. Paclitaxel spirulina nanoparticle formulation may have higher bioavailability and longer sustainable therapeutic time as compared with pure paclitaxel. Conclusion: Paclitaxel-Spirulina co-loaded nanoparticles could be effectively useful in gastric cancer as chemotherapeutic formulation.

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Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

Asian Journal of Pharmacy and Technology ◽

10.52711/2231-5713.2021.00016 ◽

2021 ◽

pp. 97-104

Author(s):

Kumara Swamy S ◽

Ramesh Alli

Keyword(s):

Drug Release ◽

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Oral Delivery ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Sustained Drug Release ◽

Bioavailability Enhancement ◽

Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

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Pharmaceutical Cocrystals: A Novel Approach for Oral Bioavailability Enhancement of Drugs

Critical Reviews in Therapeutic Drug Carrier Systems ◽

10.1615/critrevtherdrugcarriersyst.v29.i3.10 ◽

2012 ◽

Vol 29 (3) ◽

pp. 183-218 ◽

Cited By ~ 30

Author(s):

Renu Chadha ◽

Anupam Saini ◽

Poonam Arora ◽

Swati Bhandari

Keyword(s):

Oral Bioavailability ◽

Bioavailability Enhancement ◽

Pharmaceutical Cocrystals ◽

Novel Approach

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RECENT APPROACHES OF SOLID DISPERSION: A NEW CONCEPT TOWARD ORAL BIOAVAILABILITY SABITRI BINDHANI* , SNEHAMAYEE MOHAPATRA

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i2.23161 ◽

2018 ◽

Vol 11 (2) ◽

pp. 72 ◽

Cited By ~ 2

Author(s):

Sabitri Bindhani ◽

Snehamayee Mohapatra

Keyword(s):

Solid Dispersion ◽

Relative Bioavailability ◽

Review Article ◽

Water Soluble ◽

Advanced Technology ◽

Minimum Level ◽

Bioavailability Enhancement ◽

The Past ◽

Poorly Soluble

Solid dispersion (SD) has been a major advanced technology in overcoming dissolution and bioavailability problem of poorly soluble compounds. Formulation of SD in water-soluble carrier has becoming more researched over the past four decades for solubility and relative bioavailability enhancement. By reduction of the size of the drug particle to the minimum level which will enhance drug wettability and ultimately bioavailability will be definitely improved. This review article elaborates recent advanced technology and characterization of SDs and also discusses the problems and their solution for the development of better formulations.

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