Applications of innovative technologies to the delivery of antipsychotics.

The oral route is a highly recommended route for the delivery of a drug. But most lipophilic drugs are difficult to deliver via this route due to their low aqueous solubility. Selfemulsifying drug delivery systems (SEDDS) have emerged as a potential approach of increasing dissolution of a hydrophobic drug due to spontaneous dispersion in micron or nano sized globules in the GI tract under mild agitation.The main motive of this review article is to describe the mechanisms, advantages, disadvantages, factors affecting, effects of excipients, possible mechanisms of enhancing bioavailability, and evaluation of self-emulsifying drug delivery systems.Self emulsifying systems incorporate the hydrophobic drug inside the oil globules, and a monolayer is formed by surfactants to provide the low interfacial tension, which leads to improvement in the dissolution rate of hydrophobic drugs. The globule size of self-emulsifying systems depends upon the type and ratio of excipients in which they are used. The ternary phase diagram is constructed to find out the range of concentration of excipients used. This review article also presents recent and updated patents on self-emulsifying drug delivery systems. Self-emulsifying systems have the ability to enhance the oral bioavailability and solubility of lipophilic drugs.This technique offers further advantages such as bypassing the first pass metabolism via absorption of drugs through the lymphatic system, easy manufacturing, reducing enzymatic hydrolysis, inter and intra subject variability, and food effects. 

A Comprehensive Insight on Self Emulsifying Drug Delivery Systems

Design and evaluation of combined atorvastatin and ezetimibe optimized self- nano emulsifying drug delivery system

ABSTRACT Introduction Drug delivery systems (DDSs) formed by natural active compounds be instrumental in developing new green excipients and novel DDS from natural active compounds (NACs). ‘Unification of medicines and excipients’(UME), the special inherent nature of the natural active compounds, provides the inspiration and conduction to achieve this goal. Areas covered This review summarizes the typical types of NACs from herbal medicine, such as saponins, flavonoids, polysaccharides, etc. that act as excipients and their main application in DDS. The comparison of the drug delivery systems formed by NACs and common materials and the primary formation mechanisms of these NACs are also introduced to provide a deepened understanding of their performance in DDS. Expert opinion Many natural bioactive compounds, such as saponins, polysaccharides, etc. have been used in DDS. Diversity of structure and pharmacological effects of NACs turn out the unique advantages in improving the performance of DDSs like targeting ability, adhesion, encapsulation efficiency(EE), etc. and enhancing the bioavailability of loaded drugs.

Unification of medicines and excipients: The roles of natural excipients for promoting drug delivery

Aim: The aim of the present study was to develop a self-nanoemulsifying drug delivery system (SNEDDS) for the oral delivery of aripiprazole (APZ), an antipsychotic drug used in the treatment of schizophrenia. Objectives: In this investigation, attempts were made to enhance the aqueous solubility of APZ through SNEDDS and to assess its effect on oral bioavailability (BA) in rabbit. Materials and Methods: Self-emulsifying drug delivery systems of APZ were formulated with Anise essential oil as oil phase, Gelucire 44/14 as surfactant, and Transcutol HP as cosurfactant after screening various vehicles. Drug-excipient interactions were studied by Fourier transform infrared analysis. The formulations were evaluated for self-emulsifying ability, clarity, and stability of their aqueous dispersion after 48 h, and phase diagram was constructed to optimize the system. Selected formulations were characterized in terms of droplet size distribution, zeta potential, and cloud point and subjected to in vitro drug release studies. The BA of optimized formulation was assessed in Rabbits. Results and Discussion: The formulation was optimized by considering smaller droplet size, higher zeta potential, and faster rate of drug release and found to be robust to different pH media and dilution volumes and remained stable after three freeze-thaw cycles and stored at 4°C and 25°C for at least 3 months without showing significant change in droplet size. The pharmacokinetic study in rabbits showed that SNEDDS has significantly increased the area under the curve. Conclusion: SNEDDS can be effective oral dosage form for enhancing aqueous solubility and thereby improving oral BA of poorly water-soluble drug, APZ.

/pdf/formulation-development-and-bioavailability-assessment-of-3hrhjusudn.pdf

Formulation Development and Bioavailability Assessment of Aripiprazole by Self-Nanoemulsifying Drug Delivery Systems

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Formulation Development and Bioavailability Assessment of Aripiprazole by Self-Nanoemulsifying Drug Delivery Systems