Self-Nanoemulsifying Lyophilized Tablets for Flash Oral Transmucosal Delivery of Vitamin K: Development and Clinical Evaluation

Abstract

Owing to limited solubility, vitamin K undergoes low bioavailability with large inter-individual variability after oral administration. This article aimed to prepare self-nanoemulsifying lyophilized tablets (SNELTs) for the flash oral transmucosal delivery of vitamin K. Twenty-one formulae of vitamin K self-nanoemulsifying drug delivery systems (SNEDDS) were prepared using different concentrations of vitamin K, Labrasol, and Transcutol according to mixture design. The SNEDDS was loaded on porous carriers and formulated as lyophilized tablets. The release profile and the pharmacokinetic parameters of vitamin K SNELTs were evaluated in comparison with commercial tablets and ampoules on human volunteers. Results revealed that the optimized SNEDDS showed the smallest and most stable nanoemulsion globules. SNELTs were prepared successfully and showed substantial superiority drug release compared with the commercial tablets. Interestingly, SNELTs enhanced both rate and extent of vitamin K absorption as well as relative bioavailability (169.67%) in healthy subjects compared with the commercial tablets. SNELTs revealed promising no significant difference in the area under the curve compared with the commercial intramuscular injection. SNELTs enhanced dissolution and bioavailability that expected to have the strong impact on the efficiency of vitamin K in the prophylaxis and treatment of bleeding disorders in patients with hepatic dysfunction.

RETRACTED: Omega-3 Self-Nanoemulsion Role in Gastroprotection against Indomethacin-Induced Gastric Injury in Rats

“…Omega-3 SNEDDS globule size was determined by a dynamic light scattering technique utilizing a Nano-ZS particle size analyzer (Malvern Instrument, Worcestershire, UK), using 100 µL of each omega-3 SNEDDS, diluted with 10 mL of 0.1 N HCl, vortexed for 1 minute, then measured [24].…”

RETRACTED: Attenuation of Benign Prostatic Hyperplasia by Optimized Tadalafil Loaded Pumpkin Seed Oil-Based Self Nanoemulsion: In Vitro and In Vivo Evaluation

“…upper limit), takes place. Besides enhancing stability, these lipid-based nano-entities employed as novel drug delivery systems (DDSs) are indicated to improve drug solubility, dissolution behavior in the GIT, and thus are known to increase the absorption of the poorly water-soluble drugs [28][29][30][31][32].…”

“…Similar results obtained in vivo would indicate the significance of this compound as a supportive treatment for conditions, such as BPH, which frequently occurs in males aged 50 and over [25][26][27].Self nano-emulsified drug delivery systems (SNEDDSs) are increasingly being utilized in the pharmaceutical field as a vehicle or drug delivery system in various formulations, such as creams, foams, liquids, and sprays. This is because of their high degree of drug permeation through tissues, stability, and fewer side effects compared to other modern drug delivery systems [28][29][30][31][32]. SNEDDSs are superior to microemulsion because of their smaller size, larger surface area, and absence of any inherent creaming, flocculation, coalescence, or sedimentation.…”

Systematic Development of Self-Nanoemulsifying Liquisolid Tablets to Improve the Dissolution and Oral Bioavailability of an Oily Drug, Vitamin K1

“…Recently, a SNEDDS lyophilized tablets were reported for oral transmucosal delivery of vitamin K. SNEDDS was added to gelatine solution to form nanoemulsion and then freeze-dried [ 35 ]. In our research, the L-SNEDDS was solidified by liqusolid method and compressed directly into tablets.…”