Formulation self nano emulsifying drug delivery system glimepiride using oleic acid as oil phase

Patients with beta-thalassaemia major need blood transfusion frequently during their whole life. However, frequent transfusions will eventually lead to the accumulation of trivalent iron, resulting in iron overload. To reduce iron overload, patients are administered regularly with intravenous or subcutaneous infusion of deferioxamine mesylate (DFO). Nevertheless, high costs of medication, poor patient compliance, and side effects limit its use and patient's acceptance. To overcome such drawbacks, we developed a novel transdermal delivery system to administer the DFO instead of traditional injections. We assayed the feasibility of fabricating a transdermal DFO patch using the single-layer drug-in-adhesive drug delivery system. We used the pressure-sensitive adhesives and hydrogels as the drug reservoirs and studied the release profile of DFO from the transdermal patches in vitro. In order to enhance the transdermal delivery rate, chemical enhancers, polysorbate 80 and oleic acid, and physical enhancer, ultrasound, were incorporated into the monolith DFO patches. Experimental results showed that the combination of polysorbate 80 and oleic acid in the pressure-sensitive adhesives enhanced the penetration efficiency through nude mice skin. The pretreatment of nude mice skin with ultrasound temporally changed the diffusional resistance and facilitated DFO penetration through the skin. We expect that the new delivery system can enable the drug to penetrate through skin at a stable rate and reach the circulation system successfully, thus allowing the concentration of drug to achieve the therapeutic effect.

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Oleic acid based heterolipid synthesis, characterization and application in self-microemulsifying drug delivery system

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2012.01.004 ◽

2012 ◽

Vol 425 (1-2) ◽

pp. 9-18 ◽

Cited By ~ 35

Author(s):

Rahul S. Kalhapure ◽

Krishnacharya G. Akamanchi

Keyword(s):

Drug Delivery ◽

Oleic Acid ◽

Drug Delivery System ◽

Delivery System

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Improved oral bioavailability of propranolol in healthy human volunteers using a liver bypass drug delivery system containing oleic acid

International Journal of Pharmaceutics ◽

10.1016/0378-5173(92)90342-y ◽

1992 ◽

Vol 88 (1-3) ◽

pp. 423-432 ◽

Cited By ~ 21

Author(s):

S.G. Barnwell ◽

T. Laudanski ◽

M.J. Story ◽

C.B. Mallinson ◽

R.J. Harris ◽

...

Keyword(s):

Drug Delivery ◽

Oleic Acid ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability ◽

Healthy Human ◽

Human Volunteers

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FORMULATION AND EVALUATION OF LIPID BASED SELF EMULSIFYING DRUG DELIVERY SYSTEM OF GLIMEPIRIDE

INDIAN DRUGS ◽

10.53879/id.50.11.p0048 ◽

2013 ◽

Vol 50 (11) ◽

pp. 48-51

Author(s):

K Sneha Latha ◽

◽

G. B Kiran Kumar ◽

G. A Mohammed ◽

S.K Chowdary ◽

...

Keyword(s):

Drug Delivery ◽

Oleic Acid ◽

Drug Release ◽

Dissolution Rate ◽

Drug Delivery System ◽

Delivery System ◽

Classification System ◽

Tween 80 ◽

Low Solubility ◽

Biopharmaceutical Classification System

Aim of the present investigation was to develop lipid based self-emulsifying drug delivery system (SEDDS) to improve bioavailability of glimepiride. Glimepiride is a class II molecule according to BCS (Biopharmaceutical Classification System), having low solubility. Optimized self-emulsifying drug delivery system of glimepiride comprising oil (oleic acid), surfactant (Tween 80®) and co-surfactant (PEG 200®) was prepared. Optimized SEDDS of glimepiride showed increase in dissolution rate. It was concluded that the formulation was found to be showing significant improvement in terms of the drug release with complete release of drug within 18 minutes. Thus, self-emulsifying formulation of glimepiride was successfully developed.

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Formulasi Self-Nanoemulsifying Drug Delivery System (SNEDDS) Ekstrak Biji Ramania (Bouea macrophylla Griff) dengan Asam Oleat (Oleic Acid) sebagai Minyak Pembawa

Proceeding of Mulawarman Pharmaceuticals Conferences ◽

10.25026/mpc.v8i1.334 ◽

2018 ◽

Vol 8 ◽

pp. 276-284

Author(s):

Vinny Indriani ◽

Novita Eka Kartab Putri Tobing ◽

Laode Rijai

Keyword(s):

Drug Delivery ◽

Oleic Acid ◽

Drug Delivery System ◽

Delivery System ◽

Tween 20

Ekstrak biji B.macrophylla memiliki aktivitas antioksidan yang kuat namun memiliki kelarutan dan bioavailabilitas yang rendah. Meningkatkan efektivitas ekstrak biji B.macrophylla dilakukan dengan memformulasikan ke dalam sistem SNEDDS menggunakan Asam Oleat sebagai minyak pembawa. Hasil penelitian menunjukkan bahwa komposisi formula SNEDDS ekstrak biji B.macrophylla yang paling optimal terdiri dari kombinasi tween 20 : propilenglikol : asam oleat (0,5 : 3 : 1,5 dan 0,5 : 3,38 : 1,12) dalam 5 mL yang memiliki emulsification time dengan rerata waktu 19,03 detik dan 15,2 detik; nilai transmitansi 92,8% dan 94,2%; ukuran tetesan 176,8 nm dan 161,1 nm; polidisperse index 0,357 dan 0,364; serta nilai nilai IC50 ektrak biji B.macrophylla 1,757 μg/mL.

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Preparation and in-vitro evaluation of cilostazol self-emulsifying drug delivery system

Al Mustansiriyah Journal of Pharmaceutical Sciences ◽

10.32947/ajps.20.01.0436 ◽

2020 ◽

pp. 13-30

Keyword(s):

Drug Delivery ◽

Oleic Acid ◽

Drug Delivery System ◽

Delivery System ◽

Tween 80 ◽

Water Soluble ◽

In Vitro Dissolution ◽

Dissolution Profile ◽

Phosphodiesterase Iii Inhibitor

This work reported a first liquid self-nanoemulsifying drug delivery system (SEDD) of cilostazol using oleic acid as oil phase, tween 80 as surfactant, and transcutol as co-surfactant. Cilostazol is a poor water-soluble phosphodiesterase III inhibitor, which has antiplatelet and vasodilator effect used to relief intermittent claudication symptoms. Cilostazol solubility was determined in various oils, surfactants and co-surfactants and phase diagram was constructed at different oil: surfactant: co-surfactant ratios to determine the existence of nano-emulsion region. The in-vitro dissolution profile showed an optimized cilostazol SEDD formula (LT1) containing oleic acid (10%) as oil, tween 80 (45%) as surfactant, and transcutol (45%) as co-surfactant in comparison with the commercial conventionally Tablets. The LT1 formula was thermodynamically sTable, with a zeta potential of -30.48 mV and droplet size 154 nm. The LT1 capsule showed a superior dissolution profile (100%) when compared to the commercial Tablet (64%) of cilostazol. The objective of the present study is to formulate cilostazol as an oral liquid SEDD with better solubility and drug release to overcome a variable bioavailability of the commercial Tablet in which a high-fat meal increases absorption to approximately 90%.

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