Pharmacokinetic and pharmacodynamic studies of iloperidone-loaded lipid nanoemulsions via oral route of administration

Narala, Arjun; Suram, Dinesh; Veerabrahma, Kishan

doi:10.1080/03639045.2021.1908332

Cited by 4 publications

(2 citation statements)

References 27 publications

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“…Iloperidone is another atypical antipsychotic drug that acts as an antagonist for both dopamine D2 and serotonin 5-HT2 receptors, having been approved for schizophrenia treatment by the FDA in 2009. It is available as oral tablets, but extensive first-pass metabolism leads to low bioavailability, and it also has poor water solubility (predictably 0.0304 mg/mL) [ 30 , 50 ]. To help solve these issues, Narala et al developed an O/W nanoemulsion, for oral administration, containing soybean oil (Lipoid), egg lecithin (egg phosphatidyl choline, EPC80), cholesterol, oleic acid, glycerol and water (detailed quantities in Table 6 ).…”

Section: Nanometric Emulsions Containing Antipsychotic Drugsmentioning

confidence: 99%

Antipsychotics-Loaded Nanometric Emulsions for Brain Delivery

2022

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Antipsychotic drugs have numerous disabling side effects, and many are lipophilic, making them hard to formulate at high strength. Incorporating them into nanometric emulsions can increase their solubility, protect them from degradation, and increase their brain delivery, being a promising strategy to overcome the current treatment gap. A thorough review was performed to assess the true potential of these formulations for antipsychotic drugs brain delivery. Intranasal administration was preferred when compared to oral or intravenous administration, since it allowed for direct brain drug transport and reduced systemic drug distribution, having increased efficacy and safety. Moreover, the developed systems increased antipsychotic drug solubility up to 4796 times (when compared to water), which is quite substantial. In the in vivo experiments, nanometric emulsions performed better than drug solutions or suspensions, leading to improved brain drug targeting, mainly due to these formulation’s excipients (surfactants and cosolvents) permeation enhancing capability, added to a small droplet size, which leaves a large surface area available for drug absorption to occur. Thus, even if it is difficult to conclude on which formulation composition leads to a best performance (high number of variables), overall nanometric emulsions have proven to be promising strategies to improve brain bioavailability of antipsychotic drugs.

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Section: Nanometric Emulsions Containing Antipsychotic Drugsmentioning

confidence: 99%

Antipsychotics-Loaded Nanometric Emulsions for Brain Delivery

2022

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“…Innovative formulation platforms and tactics for novel oral drug delivery technologies are rapidly being developed to address this issue and increase therapeutic efficacy and safety 5,6 . The range of nano-systems in the oral drug delivery area includes liposomes 7,8 , solid lipid nanoparticles 9,10 , nanocrystals [11][12][13] , liposomes 8,14 , polymeric nanoparticles [15][16][17] which are obtained via specialized techniques such as high pressure homogenizer (HPH) 18,19 . Typically, nano-systems exhibits stability issues caused by agglomeration 20 .…”

Section: Introductionmentioning

confidence: 99%

A Review on Hot Melt Extrusion Coupled Novel Drug Delivery Systems

Parvathaneni¹,

Battu

Sudhakar

2022

J. Drug Delivery Ther.

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The utilization of hot melt extrusion (HME) technology for new applications is increasing in recent years, as evidenced by the many published reports in the last five years. Because of its process automation and low-cost scale-up qualities, which decrease labor expenses and capital investment. HME has emerged as an essential technology for drug delivery applications in pharmaceutical research and manufacture. The novel application of the HME process provides a promising alternate approach in the formulation of novel drug delivery systems. The present review discusses the importance of HME in the development of novel drug delivery systems with the review of relevant case studies. Keywords: hot melt extrusion, novel drug delivery, pharmaceutical research

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