Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation

Baek, Myoungki; Lee, Jong-Hwa; Cho, Young-Ho; Kim, Hak-Hyung; Lee, Gye-Won

doi:10.2147/ijn.s37338

Cited by 17 publications

(3 citation statements)

References 33 publications

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“…It was demonstrated that the particle size of SMEDDS may be affected by the substances in the medium during the dissolution study [ 37 ]. In the dissolution medium, we discovered F35 could further self micro-emulsify into larger nano-level droplets in the RPMI medium compared to the SIFsp medium ( Table 1 ).…”

Section: Discussionmentioning

confidence: 99%

Oleic Acid-Based Self Micro-Emulsifying Delivery System for Enhancing Antifungal Activities of Clotrimazole

et al. 2022

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Due to the increasing rate of drug resistance in Candida spp., higher doses of antifungal agents are being used resulting in toxicity. Drug delivery systems have been shown to provide an effective approach to enhance the efficacy and reduce the toxicity of antifungal agents. Oleic acid was revealed to effectively inhibit biofilm formation, hence reducing the virulence of Candida albicans. In this study, oleic acid-based self micro-emulsifying delivery systems (OA-SMEDDS) were developed for delivering clotrimazole (CLT). Based on the pseudo-ternary phase diagram and loading capacity test, the optimal ratio of OA-SMEDDS with CLT was selected. CLT-loaded OA-SMEDDS not only bears a higher drug loading capacity but also maintains good storage stability. The minimum inhibitory concentration (MIC50) of CLT-loaded OA-SMEDDS (0.01 μg/mL) in Candida albicans was significantly lower than that of CLT dissolved in DMSO (0.04 μg/mL). Moreover, we showed CLT-loaded OA-SMEDDS could effectively prevent biofilm formation and destroy the intact biofilm structure of Candida albicans. Furthermore, a CLT-loaded OA-SMEDDS gel was developed and evaluated for its antifungal properties. Disk diffusion assay indicated that both CLT-loaded OA-SMEDDS and CLT-loaded OA-SMEDDS gels were more effective than commercially available products in inhibiting the wild-type and drug-resistant species of Candida.

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Section: Discussionmentioning

confidence: 99%

Oleic Acid-Based Self Micro-Emulsifying Delivery System for Enhancing Antifungal Activities of Clotrimazole

et al. 2022

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“…Twelve rats were randomly divided into two groups (ZgI and ZgI-SMEDDS) of six rats each and were housed in IVC animal house and lighted on a regular 12-h light-dark cycle. The methods for the SPIP studies were carried out according to references (20,21). Briefly, 10% chloral hydrate (4.0 mL/kg) was i.p-injected to anesthetize rats; then, rats were placed on a heating operating table to maintain a body temperature of 37°C.…”

Section: Methodsmentioning

confidence: 99%

Development and In Vivo Evaluation of Ziyuglycoside I–Loaded Self-Microemulsifying Formulation for Activity of Increasing Leukocyte

et al. 2019

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Ziyuglycoside I (ZgI), a major effective ingredient of Sanguisorba officinalis L, has shown good activity in increasing leukocyte of myelosuppression mice. However, oral ZgI therapy has been deterred by poor bioavailability because of its low aqueous solubility and permeability. Our study was to develop ZgI-loaded self-microemulsifying drug delivery system (SMEDDS) and evaluate its intestinal absorption, and pharmacokinetic and pharmacodynamic activity for increasing leukocyte. The formulation was designed and optimized by measuring the equilibrium solubility of ZgI in different vehicles and the pseudoternary phase diagram. Further, morphology, particle size, stability, in vitro release, in situ single-pass intestinal perfusion (SPIP), in vivo activity, and in vivo pharmacokinetic (PK) of ZgI-SMEDDS were charactered or studied. Optimized formulations for in vitro dissolution were Obleique CC497, Tween-20, and Transcutol HP with a proportion of 0.25/0.45/0.30 via D-optimal mixture design. Results showed that the solubility of ZgI was enhanced up to 23.93 mg/g and its average particle size was 207.92 ± 2.13 nm. The release of ZgI had been greatly improved by the SMEDDS. In SPIP, the intestinal absorption of SMEDDS was much better than plain ZgI. In PK, we found the oral bioavailability of ZgI-SMEDDS was 6.94-fold higher absolute bioavailability (21.94 ± 4.67) % than ZgI (3.16 ± 0.89) %. The most important was that the mice WBC of ZgI-SMEDDS group was significantly higher than that of the ZgI group. Our study suggested that SMEDDS could increase the solubility of ZgI, which was beneficial to improve oral bioavailability and enhance biological activity.

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“…L-SMEDDS promotes drug absorption via intestinal lymph by passing the firstpass impact of drugs. Moreover, drug added with the aid of using L-SMEDDS can spontaneously shape micro-emulsion with a droplet size of dozens of nanometers inside the gastrointestinal tract after oral administration 13,14,15,16 and, therefore, enhances the absorption and bioavailability of poorly waters soluble drugs 17 . Despite many advantages, L-SMEDDS also have some significant drawbacks, including long-time stability issues, storage, transportation inconvenience, and irreversible drug precipitation 18 .…”

Section: Introductionmentioning

confidence: 99%

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2022

IJPSR

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SMEDDS are formulated to improve the oral bioavailability of lipophilic drugs. It is an isotropic mixture of compounds like oil, surfactant, co-surfactant, and drug having the unique ability to form fine o/w micro-emulsion by agitation and diluted with GI fluid. Its liquid formulation technique enhanced the absorption and bioavailability of poorly watersoluble drugs but also had a few drawbacks like long time period stability issues and storage conditions. Some special techniques convert the liquid form into solid dosage form to overcome these problems. The present paper gives exhaustive information about formulation design by screening excipients. We study the selection and solubility of excipients, its preparation and characterization, and the mechanism by which bioavailability can be improved. This discussion is useful for a better understanding of SMEDDS for its recent advancements, marketed formulation, and patents on SMEDDS. The poorly water-soluble drugs having dissolution rate absorption limited can be effectively formulated in the form of SMEDDS causing a stable plasma profile. The plasma levels of the poorly aqueous soluble medicament show the critical passage of drug absorption, i.e., dissolution. Surfactants with a high HLB value, such as Tween 80 are said to increase the permeability of active ingredients when administered in conjunction with the formulation due to their loosening effect on tight junctions.

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Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation

Cited by 17 publications

References 33 publications

Oleic Acid-Based Self Micro-Emulsifying Delivery System for Enhancing Antifungal Activities of Clotrimazole

Oleic Acid-Based Self Micro-Emulsifying Delivery System for Enhancing Antifungal Activities of Clotrimazole

Development and In Vivo Evaluation of Ziyuglycoside I–Loaded Self-Microemulsifying Formulation for Activity of Increasing Leukocyte

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