Preparation and properties of a stable intravenous lorazepam emulsion

Abstract

Lorazepam is normally administered as a solution in organic solvents such as propylene glycol. This type of formulation is undesirable. This study describes the development of a parenteral emulsion formulation for lorazepam. The stability of lorazepam in the emulsion was examined. Ten per cent corn oil emulsions stabilized with egg lecithin, Pluronic F68 and Pluronic F88 were used. The incorporation of lorazepam does not appear to destabilize the emulsion, and lorazepam itself appears to be stable for at least 1 year in this liquid formulation. Haemolysis caused by emulsion formulations containing lorazepam and different emulsifiers was evaluated using human and rabbit blood to assess their safety as parenteral drug carriers. The results show that the emulsions did not have any significant haemolytic activity whereas organic solvents and solutions of lorazepam in organic solvents caused substantial haemolysis.

Development and Evaluation of Lorazepam Microemulsions for Parenteral Delivery

“…Furthermore, parenteral administration of the organic cosolvents can also cause hemolysis. Yalin et al, (4) observed that the conventional LZM solution results in considerable in vitro hemolysis of human and rabbit blood (>80%). Hence, it is desirable to develop a suitable parenteral dosage form of LZM using novel delivery approaches.…”

“…Hence, it is desirable to develop a suitable parenteral dosage form of LZM using novel delivery approaches. Researchers have explored the potential of emulsions (4,5) and cyclodextrins (1) in improved parenteral delivery LZM. However, both these approaches have their own limitations.…”

In vivo gene delivery into ocular tissues by eye drops of poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) (PEO-PPO-PEO) polymeric micelles

“…Recently, a non-ionic PEO-PPO-PEO copolymer with an average molecular weight of 8400, a group of triblock copolymers derived from propylene oxide (20%) and ethylene oxide (80%), 6 have been widely used in medical, pharmaceutical, and cosmetic systems as a solubilizing, wetting, and emulsifying agent with relatively low toxicity. 7,8 In addition, there are many nano-polymeric micelle drug systems which contain hydrophilic PEO chains as palisade regions, can prohibit protein/serum absorption in vitro, 9 liver cellular interaction, and can increase stability in the blood stream. 10 This PEO-type carrier of block copolymer not only leads to enhanced passive transport but also avoids liver degradation.…”

A Recent Review on Nasal Microemulsion for Treatment of CNS Disorder

“…Co-solvent based parenteral formulations, however, have several disadvantages, such as pain and tissue damage at the site of injection and precipitation of the drug on dilution in several cases [41]. Furthermore, parenteral administration of the organic co-solvents can also cause hemolysis [42]. Amit et al, Prepared lorazepam microemulsions and demonstrated that microemulsion has very low hemolytic potential and exhibit good physical and chemical stability and can be considered as a viable alternative to the currently marketed lorazepam formulations [43].…”