Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, <i>in vitro</i> Characterization and <i>ex vivo</i> Intestinal Permeation Study

Abstract

IntroductionDiabetes type 2, diabetes mellitus is a group of metabolic disease in which the blood glucose level increase ≥ 200 mg/dL for a long period. Due to high blood glucose level, many other symptoms appeared simultaneously like more frequent urination, weight loss, increased hunger, dehydration, as well as the alteration in lipid profile, liver function test and kidney function test. The associated complication may occur like heart attack, kidney failure and damaged eye in chronic and serious condition. In worldwide approx. 422 million peoples were affected and about 1.6 million deaths occurred in the low and middle-income countries in every year 1 . Various oral dosage form available in the market to reduce the blood glucose level

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

“…This may be due to the fact that after oral administration of IVA-SNEDDS, IVA-SNEDDS can form a nanoemulsion under the slight peristalsis of the gastrointestinal tract, and the nanoemulsion increases the absorption area of IVA in the gastrointestinal tract. 60 In addition, the drug is dissolved in the oil phase and is located in the core of the nanoemulsion, which is not affected by environmental changes such as pH, ions, and food in the gastrointestinal tract, and can also reduce the degradation effect of enzymes on it. 61 …”

Drug delivery systems as immunomodulators for therapy of infectious disease: Relevance to COVID-19

“…The potential of the SGLT2 inhibitor dapagliflozin is currently being tested in two phase 3 trials, DARE-19 (NCT04350593) and TACTIC-E (NCT04393246), to assess if there can be an improvement on clinical recovery and respiratory complications for non-critically ill patients, who are hospitalised due to COVID-19 [199] , [200] . Dapagliflozin has been nanoformulated with the intention to control diabetes [201] , which could also be utilised for use for the treatment of COVID-19, with an increased permeability [202] , optimal drug release profile in simulated gastric fluid and improved oral hypoglycaemic activity [201] .…”

Olive Leaves (<i>Olea europaea</i> L) Extract Loaded Lipid Nanoparticles: Optimization of Processing Parameters by Box-Behnken Statistical Design, <i>in-vitro</i> Characterization, and Evaluation of Anti-oxidant and Anti-microbial Activity

“…screening study and pre-optimization of formulation variables For the selection of suitable lipid, surfactant, homogenization speed & time, sonication time, etc., preliminary studies were conducted 32,33) . The selection of suitable lipid depends upon the drug solubility in lipid and selection of surfactant is depending upon the solubility of lipid in surfactant.…”

“…On the other hand, surfactant (1.5-4.5％) exhibited a negative effect on the particle size (Table 1, batch F1 237.05 nm and F3 112.35 nm) . This might be due to a decrease in interfacial tension between the aqueous and lipid phase which prevents particle aggregation 33) . Homogenization speed exhibited a negative impact (Table 1, batch F5 187.46 nm and F7 134.27 nm) on the particle size due to the generation of high force which breaks the particles and hence reduces the particle size.…”