Design and development of a self-microemulsifying drug delivery system of olmesartan medoxomil for enhanced bioavailability

Komesli, Yelda; Ozkaya, Ali Burak; Ergur, Bekir Uğur; Kirilmaz, Levent; Karasulu, Ercüment

doi:10.1080/03639045.2019.1607868

Cited by 21 publications

(12 citation statements)

References 58 publications

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“…SEDDS can be divided into self-micro-emulsifying drug delivery systems and self-nanoemulsifying drug delivery systems, according to the size of the self-emulsified droplets (Kohli et al., 2010 ). The numerous advantages of SEDDSs, including their physical stability, simple manufacturing process, and oral application via soft or hard gelatin capsules explain why they have been researched intensively within the last few decades (Gupta et al., 2013 ; Yeom et al., 2017 ; Komesli et al., 2019 ; Fidan et al., 2022 ). A renowned alternative approach for the delivery of drugs with low water solubility is using lipid formulations, particularly SEDDS, that deal with low aqueous solubility and poor oral bioavailability (Almeida & Tippavajhala, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

The preparation and relative bioavailability of an artemisin in self-emulsifying drug delivery system

et al. 2023

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The aim of this study is to demonstrate a method for improving the solubility and relative bioavailability of artemisinin using a self-emulsifying drug delivery system (SEDDS). The self-emulsifying drug load, solubility, and emulsifying time were used as the evaluation indices, based on a solubility test and a ternary phase diagram. Optimal Mixture Design in Design-Expert software was used to optimize the prescription of the artemisinin SEDDS. By determining the water distribution coefficient in vitro, combined with the drug concentration–time curve in vivo , a comparison was made of the relative oral bioavailability of the artemisinin SEDDS and the crude drug. The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the artemisinin SEDDS was 0.5:0.2:0.3 (wt/wt/wt), with a drug loading capacity of 41.556 mg/g, a solubility of 1.997 mg/mL, and a self-emulsification time of 214 s. The optimal prescription was transparent, slightly yellow, and oil-like. The average loading capacity of artemisinin was 41.912 mg/g, the emulsification time was 231 s, the average particle size was 128.0 nm, the average Zeta potential was –4.29 mV, and the solubility of artemisinin SEDDS in water was 1.997 mg mL –1 . It is 33.85 times of the solubility of artemisinin in water, which achieves the purpose of increasing the solubility of artemisinin. The comparison of the oil/water distribution coefficient of the artemisinin SEDDS with that of the crude drug in vitro showed that SEDDS could improve the permeability of artemisinin and promote the absorption in vivo , and the relative bioavailability of the SEDDS agent was at least 1.47 times higher than that of the crude drug. The artemisinin SEDDS could significantly improve the solubility and relative bioavailability of artemisinin.

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Section: Introductionmentioning

confidence: 99%

The preparation and relative bioavailability of an artemisin in self-emulsifying drug delivery system

et al. 2023

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“…Rats were randomly divided into seven groups ( n = 8) including the normal control (NC) group, TNBS-colitic (positive control, PC) group, and five TNBS-colitic-treated groups which were orally given sulfasalazine (SSZ, 100 mg/kg/day, a reference treatment for IBD) (Yousefi-Ahmadipour et al., 2020 ), low and high doses of OM (OML and OMH: 3.0 and 10.0 mg/kg/day (Nagib et al., 2013 )) as a raw drug and as an OMS (OMSL and OMSH). OM was suspended in distilled water containing 0.25% carboxymethyl cellulose (Gorain et al., 2014 ; Komesli et al., 2019 ). The treatments were given for 7 days starting 4 hours after TNBS administration (Lu et al., 2017 ).…”

Section: Methodsmentioning

confidence: 99%

“…But unfortunately, it has low bioavailability due to its highly lipophilic nature and efflux by gut drug resistance pumps (Kobayashi et al., 2000 ). This low bioavailability was enhanced by a self-micro emulsifying drug delivery system (SMEDDS) which is an OM lipophilic formulation rapidly absorbed from the intestine and hence does not cause sprue-like enteropathy; which could occur as a side effect of the regular OM (Komesli et al., 2019 ). OM was reported to have protective, anti-inflammatory, and antioxidant effects in dextran sodium sulfate (DSS)-induced colitis and acetic acid-induced colitis in rats (Nagib et al., 2013 ; Saber et al., 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Olmesartan medoxomil self-microemulsifying drug delivery system reverses apoptosis and improves cell adhesion in trinitrobenzene sulfonic acid-induced colitis in rats

et al. 2022

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Olmesartan medoxomil (OM) is an angiotensin receptor blocker. This study aimed to investigate the effects of OM self-microemulsifying drug delivery system (OMS) in trinitrobenzene sulfonic acid (TNBS)-induced acute colitis in rats. Besides two control groups, five TNBS-colitic-treated groups ( n = 8) were given orally sulfasalazine (100 mg/kg/day), low and high doses of OM (3.0 and 10.0 mg/kg/day) (OML and OMH) and of OMS (OMSL and OMSH) for seven days. A colitis activity score was calculated. The colon was examined macroscopically. Colonic levels of myeloperoxidase, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), malondialdehyde, and reduced glutathione were measured. Plasma and colonic olmesartan levels were measured. Colonic sections were subjected to hematoxylin and eosin staining and immunohistochemical staining for E-cadherin, caspase-3, and matrix metalloproteinase-9 (MMP-9). Protein expression of E-cadherin, Bcl-2 associated X protein (Bax), and B-cell lymphoma 2 (Bcl-2), and cleaved caspase-3 by Western blot was done. TNBS-colitic rats showed increased colonic myeloperoxidase, TNF-α, IL-6, and malondialdehyde, decreased colonic glutathione, histopathological, immunohistochemical, and protein expression alterations. OMS, compared with OM, dose-dependently achieved higher colonic free olmesartan concentration, showed better anti-inflammatory, antioxidant, and anti-apoptotic effects, improved intestinal barrier, and decreased mucolytic activity. OMS more effectively up-regulated the reduced Bcl-2, Bcl-2/Bax ratio, and E-cadherin expression, and down-regulated the overexpressed Bax, cleaved caspase-3, and MMP-9. OMSL exerted effects comparable to OMH. Sulfasalazine exerted maximal colonic protective effects and almost completely reversed colonic damage, and OMSH showed nearly similar effects with non-significant differences in-between or compared with the normal control group. In conclusion, OMS could be a potential additive treatment for Crohn's disease colitis.

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“…The experiments were carried out using our previous standardized and optimized Self microemulsifying drug delivery system (SMEDDS) with 150 nm droplet size and validated HPLC method that reported in our previous article (Komesli et al 2019). The formulation contains 14.72% Oleic acid as oil, 16.218% Tween 80 and 16.218% Span 80 as surfactant, 32.435% Transcutol as co-surfactant and 20.41% water and OM as an active ingredient.…”

Section: Preparation Of Om-smedds and Om-suspensionmentioning

confidence: 99%

“…The formulation contains 14.72% Oleic acid as oil, 16.218% Tween 80 and 16.218% Span 80 as surfactant, 32.435% Transcutol as co-surfactant and 20.41% water and OM as an active ingredient. The OM-SMEDDS was formulated at a dose of 1 mg/ml in accordance with the physicochemical properties of OM by the technique of our previous publication [109]. The OM-Suspension was obtained by suspending 0.25 g of CMC in 100 mL distilled water and adding 1 mg/ml of the active ingredient.…”

Section: Preparation Of Om-smedds and Om-suspensionmentioning

confidence: 99%

Evaluation of anti-inflammatory, immunomodulatory effects and celiac-like side effect of olmesartan medoxomil as a vitamin D receptor agonist and angiotensin II receptor blocker

Komesli¹,

Karasulu²

2022

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Design and development of a self-microemulsifying drug delivery system of olmesartan medoxomil for enhanced bioavailability

Cited by 21 publications

References 58 publications

The preparation and relative bioavailability of an artemisin in self-emulsifying drug delivery system

The preparation and relative bioavailability of an artemisin in self-emulsifying drug delivery system

Olmesartan medoxomil self-microemulsifying drug delivery system reverses apoptosis and improves cell adhesion in trinitrobenzene sulfonic acid-induced colitis in rats

Evaluation of anti-inflammatory, immunomodulatory effects and celiac-like side effect of olmesartan medoxomil as a vitamin D receptor agonist and angiotensin II receptor blocker

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