Abstract:The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release-Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L-SMEDDS) were… Show more
“…4 A depicts the differential scanning calorimetry (DSC) thermograms for NBV, Span, Labrasol, their PM, and the selected SNVs either plain or medicated. NBV thermogram showed a single sharp endothermic peak at 226.52 °C ( Trivedi et al, 2020 ). The drug's crystalline structure was revealed by its distinct peak and it corresponded to its melting point.…”
Section: Resultsmentioning
confidence: 99%
“…5 displays the release profile of NBV from a control suspension and the optimized three formulae (F1, F4, and F14). It was obvious that incorporating NBV within SNVs significantly slowed down the drug release as the vesicular system is well-known to act as a reservoir that slowly releases the drug providing a sustained release profile ( Trivedi et al, 2020 ). Fig.…”
“…4 A depicts the differential scanning calorimetry (DSC) thermograms for NBV, Span, Labrasol, their PM, and the selected SNVs either plain or medicated. NBV thermogram showed a single sharp endothermic peak at 226.52 °C ( Trivedi et al, 2020 ). The drug's crystalline structure was revealed by its distinct peak and it corresponded to its melting point.…”
Section: Resultsmentioning
confidence: 99%
“…5 displays the release profile of NBV from a control suspension and the optimized three formulae (F1, F4, and F14). It was obvious that incorporating NBV within SNVs significantly slowed down the drug release as the vesicular system is well-known to act as a reservoir that slowly releases the drug providing a sustained release profile ( Trivedi et al, 2020 ). Fig.…”
Uncontrolled diabetes is a major cause of blindness, kidney failure, heart attacks, stroke, and lower limb amputation. In 2019, diabetes was the ninth leading cause of death, with an estimated 1.5 million deaths directly caused by diabetes 1 . Sulphonylureas are a medicine used to enhance insulin release to control sugar levels in the normal range.Glibenclamide (Glb) is one of the most potent second-generation sulphonyurea (dose 2.5-20 mg) for it. Glb is highly lipophiic (pka-5.3) and BCS class II drug. This drug shows variable oral bioavailability due to poor drug solubility and dissolution. It also shows serious and sometimes fatal side effects like hypoglycemia attack and
“…The lipids are likely to augment the lymphatic transport of a lipophilic drug substance leading to enhanced oral bioavailability [8][9][10][11] . The drug, i.e., nebivolol, chosen in the present study is a BCS class II highly selective thirdgeneration β 1 -receptor antagonist, an antihypertensive drug with poor water-solubility and high permeability (log P of 4.03) undergoes rapid first-pass metabolism caused by cytochrome P450 2D6 (CYP2D6) enzymes resulted in poor bioavailability (12%) 12 . All these considerations have led to the development of solid oral SMEDDS.…”
The present investigation aimed to prepare a self micro emulsifying drug delivery system (SMEDDS) for the dissolution enhancement of nebivolol hydrochloride. The main objective of this work was to develop, characterize, and evaluate a solid SMEDDS prepared by using the adsorption technique of a liquid SMEDDS to improve the solubility and dissolution rate of nebivolol hydrochloride. The excipients were chosen based on the high solubility of nebivolol hydrochloride, and their concentrations were optimized by constructing ternary phase diagrams. Thirty-two combinations were prepared using oil (Labrafac Lipophile WL 1349), surfactant (Kolliphor RH 40), and co-surfactant (Gelucire 44/14). Self-emulsification time, dilution studies, and thermodynamic stability studies were satisfactory. The in vitro nebivolol release profile showed a faster rate of dissolution compared with the pure nebivolol hydrochloride suspension and marketed formulation. The droplet size was in the range of 132.8±22.1 to 955.7±15.5 nm and zeta potential in the range -7.2±0.53 mV to -46.4±0.32 mV for the selected formulations. Formulation N17 (Labrafac Lipophile WL 1349 -10%w/w, Kolliphor RH40-72%w/w, Gelucire 44/14- 18%w/w) was considered as optimized formulation and showed drug release of 97.26 ± 1.16% in 0.1 N HCl in 120 minutes, the particle size of 132.8±22.1 nm and zeta potential of -46.4±0.32 mV. Thus, the present studies ratify that the bioavailability was improved by nebivolol SMEDDS formulation. The optimized liquid SMEDDS was further used for the preparation of Solid SMEDDS (S-SMEDDS) formulations by using adsorption carriers. The optimized Solid SMEDDS formulation exhibited 95.38 ± 0.76% in vitro drug releases, which was significantly higher than that of the drug solution. The optimized formulation of nebivolol-loaded S-SMEDDS exhibited complete in vitro drug release in 120 min as a compared pure drug solution. The present result confirmed the potential use of SMEDDS to improve the dissolution and oral bioavailability of poorly water-soluble nebivolol.
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