Oral Bioavailability Enhancement Of Poorly Soluble And Poorly Permeable Drugs Using Self-Microemulsifying Drug Delivery Systems And The Effect Of Piperine

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dc.contributor.authorMallikarjun, Chitneni
dc.date.accessioned2018-06-08T07:39:36Z
dc.date.available2018-06-08T07:39:36Z
dc.date.issued2010-01
dc.description.abstractThere are approximately 40% of new drug molecules discovered and some drug molecules that are available in the market, having poor bioavailability due to poor solubility and/or poor permeability. The present study aimed at formulating a selfmicroemulsifying drug delivery system (SMEDDS) using two BCS class IV drugs, namely sulpiride and norfloxacin. Sulpiride is a P-gp substrate and norfloxacin is a substrate of MRP2, BCRP and an unknown efflux pump. From the solubility studies of drugs in various oils, surfactants and co-surfactants, oleic acid, Tween 80 and propylene glycol were chosen to prepare SMEDDS formulations. Two formulations were chosen for further study based on droplet size and solubility. The first formulation consisted of 4.76% w/w of oleic acid, 63.49% w/w of Tween 80 and 31.75% w/w of propylene glycol, with a mean droplet diameter of 9.27 nm and drug solubility of 22 mg/1000 mg for sulpiride, 9.57 nm and 17.33 mg/1000 mg for norfloxacin respectively. The other formulation consisted of 17.71% w/w of oleic acid, 55.14% w/w of Tween 80 and 27.15% w/w of propylene glycol, with a mean droplet diameter of 85 nm and drug solubility of 32 mg/1000 mg for sulpiride, 92 nm and 27.53 mg/1000 mg for norfloxacin. Isocratic HPLC- fluorescence methods were developed and validated for the determination of sulpiride and norfloxacin in rat intestinal perfusates and rabbit plasma separately. The in situ permeability experiment was performed on three intestinal segments, duodenum, jejunum and ileum in rats using single-pass perfusion technique. The SMEDDS formulation and micellar solution exhibited significant increase in the effective permeability coefficient of the drug across all the three intestinal segments compared with drug solution for the two drugs. There was no significant difference in the effective permeability coefficients values between SMEDDS formulation and micellar solution for both drugs.en_US
dc.identifier.urihttp://hdl.handle.net/123456789/5718
dc.language.isoenen_US
dc.publisherUniversiti Sains Malaysiaen_US
dc.subjectSelfmicroemulsifying drug delivery systemen_US
dc.subjectusing sulpiride and norfloxacinen_US
dc.titleOral Bioavailability Enhancement Of Poorly Soluble And Poorly Permeable Drugs Using Self-Microemulsifying Drug Delivery Systems And The Effect Of Piperineen_US
dc.typeThesisen_US
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