Development of solidified self-microemulsifying drug delivery systems containing l-tetrahydropalmatine: Design of experiment approach and bioavailability comparison

Tung, Nguyen-Thach; Tran, Cao-Son; Pham, Thi-Minh-Hue; Nguyen, Hoang-Anh; Nguyen, Tran-Linh; Chi, Sang-Cheol; Nguyen, Dinh-Duc; Bui, Thi-Bich-Huong

doi:10.1016/j.ijpharm.2017.12.027

Cited by 45 publications

(16 citation statements)

References 34 publications

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“…Type II formulations are often referred to as SEDDS which comprise water-insoluble components; blends of glycerides and non-ionic surfactants with HLBs less than 12 such as; polysorbate 85 (Tween 85) or polyoxyethylene 25glyceryl trioleate (Tagat TO). Type III systems contain blends of glycerides (oils), hydrophilic surfactants with HLB>12 such as; Cremophor RH40 [10,11], Cremophor EL [12,13], Tween 80 [14,15], Tween 20 [14] or Tagat O2 [16] and/or hydrophilic co-solvents such as, ethanol, propylene glycol or polyethylene glycol. Type III formulations which include water-soluble components are referred to as self-micro-emulsifying systems (SMEDDS) as they can lead to the production of a microemulsion on dispersion in GI tract (particle size ≈ 50 nm).…”

Section: Introductionmentioning

confidence: 99%

Role of Hydrophilic Surfactants in the Emulsification Mechanistics of Type Iii Self-Micro-Emulsifying Drug Delivery Systems (Smedds)

Hasan

2019

Int J App Pharm

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Objective: Evaluation of the self-emulsifying behaviour of type III lipid systems comprising mixed medium chain glycerides (Miglyol 812-Imwitor 988) and wide range of hydrophilic surfactants in an attempt to identify self-emulsifying microemulsion formulations, prevaricate the crystallization tendency of Cremophor RH40 in the pre-microemulsion concentrate, to shed some light on the mechanistic behavior of these systems after aqueous dispersion. Methods: Non-ionic surfactants with HLB in the range 14 to 16.5 are investigated amongst these are; Cremophor RH40, Cremophor EL, Crillet 4 (polysorbate 80), Crillet 1 (polysorbate 20) and Tagat O2. Optimum oil blends of Miglyol 812-Imwitor 988 and various non-ionic surfactant systems were verified using self-emulsification performance studies, oil droplet diameter measurements and dynamic equilibrium phase studies. Results: Oil blends of Miglyol 812 as an oil and Imwitor 988 as a cosurfactant were optimized for microemulsion systems at ratios of 1:1 in the case of Cremophor RH40 or EL, and at 2:3 in the case of Crillet 4 or Tagat O2. In order to obtain small droplet size and fast dispersion rate for type III lipid systems, hydrophilic surfactants with HLB values between 13 and 15 were found to be the optimum. Conclusion: Spontaneous micro-emulsification in type III lipid system was attributed to the “diffusion and stranding” theory. Yet, the formation of liquid crystalline phases as intermediate phases during dilution of the oil formulation with water appears to be quintessential for the mechanistics of emulsification regardless type of lipid class system.

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Section: Introductionmentioning

confidence: 99%

Role of Hydrophilic Surfactants in the Emulsification Mechanistics of Type Iii Self-Micro-Emulsifying Drug Delivery Systems (Smedds)

Hasan

2019

Int J App Pharm

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“…After dilution of SMEDDS with water, the impervious and milky white occurrence shows the development of macro emulsion though the fine, isotropic, clear solution shows the development of micro emulsion [36]. The preparation can be considered as constant when drug precipitation is not distinct [44]. Precipitation is normal if the preparation contains water soluble co-solvents and can be prevented by increasing the concentration of surfactant [36,45].…”

Section: (8) Characterization and Evaluation Of Smeddsmentioning

confidence: 99%

Review of formulation and evaluation of self-micro emulsifying drug delivery system (SMEDDS)

Bahadur¹,

Yadu²,

Baghel³

et al. 2020

ScienceRise: Pharmaceutical Science

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Approximately half of the new drug applicants that reach formulation have poor water solubility. Oral delivery has been the main route of drug administration for the chronic treatment of numerous diseases. In different cases, in oral conveyance, 50 % of the medication compound is hampered because of the high lipid soluble or fat soluble of the medication itself. Around 40 % of new drug applicants show low solubility in water, which prompts poor oral bioavailability, high Intra and Intersubject changeability, and deficiency of dose proportionality Aim of review. The main aim of this review article is to gather the information related to design and evaluation of SMEDDS. These information can be utilized to enhance the bioavailability of the poorly aqueous soluble drug for various types of orally administered drugs. In this review article, various literature are reviewed and summerised in single paper to serve as reference guide to various research scholars and researchers working on self-micro-emulsifying drug delivery systems. Materials and Methods. To prepare this manuscript various keywords were searched in different search engine such as Google, Yahoo and Bing etc. This review article reviews the recent work done in the field of SMEDDS. It comprises review of literatures available in public domain and formulation of SMEDDS and its characterization is summarized in this article. Result. The various strategies to developed poor aqueous soluble drug for improvement of bioavailability for example, salt development and molecular size reduction of the compound might be one technique to enhance the dissolution rate of the drug. In any case, these methods have their limitations. SMEDDS is one of the novel applications for the delivery of low water soluble and low bioavailability of drug. SMEDDS is a method to improve the aqueous solubility of the medication; SMEDDS are described as isotropic blenders of oils, surfactants, and co-surfactant. Upon slightly stir followed by dilution with distilled water, for example, gastrointestinal liquids, these techniques can define clear o/w micro emulsion. SMEDDS is first choice and key technology for developing the lipophilic drug and other different factors that chance to affect the oral bioavailability. Conclusions. This review paper attempts to describe the preparation of SMEDDS and furthermore discusses the development of pseudo ternary phase diagram for SMEDDS. It describes the mechanism and method of preparation involved in SMEDDS. The capability of oral absorption of drug compound from the SMEDDS relies upon numerous formulation−related parameters, for example, surfactant concentration, oil/surfactant ratio, and hydrophobicity of emulsion, globule size and charge, in vitro, in vivo all of which basically characterized the ability of self-emulsification. SMEDDS are administered as unit dosage form and it also protect the degradation of drug.

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“…The reason for the bioavailability enhancement of SMEDDS is that it can spontaneously form an oil‐in‐water dispersion system with diameters <100 nm under gastrointestinal peristalsis or mild stirring. In addition, the components used in SMEDDS like oil, surfactant and cosolvent were well known as solubilizers or permeability enhancers, which played a pivotal role in the enhancement of drug bioavailability (Tung et al, 2018). In order to evaluate the efficacy of the novel formulations of l ‐THP, it is essential to study its pharmacokinetics in vivo (Singh et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

“…Although earlier research described several methods for determination of l ‐THP by high‐performance liquid chromatography (HPLC) with fluorescence detection and HPLC with tandem mass spectrometry (HPLC–MS/MS) (Abdallah et al, 2017; Wang et al, 2012; Xiao et al, 2014), studies have mainly focused on l ‐THP suspension. Until now, there has been no report about the effects of different formulations of l ‐THP except one in rabbit plasma (Tung et al, 2018). In this study, a simple, selective and highly sensitive UPLC–MS/MS method has been developed and validated for the simultaneous determination of l ‐THP and l ‐ICP in rat brain.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic study of three different formulations of l‐tetrahydropalmatine in brain tissues of rats

Zhang

Huai

et al. 2021

Biomedical Chromatography

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l‐Tetrahydropalmatine (l‐THP), an active alkaloid compound isolated from Rhizoma Corydalis‐yanhusuo, has been reported to possess biological activity for treating cocaine use. To enhance both oral bioavailability and brain penetration, three formulations of l‐THP suspension, mixture of l‐THP–puerarin and self‐microemulsifying drug delivery systems (SMEDDS) were prepared. A sensitive and reliable ultra‐high‐performance liquid chromatography with tandem mass spectrometry method was developed and validated for the simultaneous determination of l‐THP and its active metabolite l‐isocorypalmine (l‐ICP) in rat brain. Diazepam was used as the internal standard. The chromatographic separation was achieved on a Bonshell ASB C18 column at 30°C using acetonitrile–aqueous formic acid as mobile phase in gradient mode. The linearity was validated over the concentration ranges of 4.00–2,500 ng/ml for l‐THP and 0.400–500 ng/ml for l‐ICP. Full method validation was within the acceptance limits. The method was successfully used to determine the pharmacokinetics of two analytes following oral administration of these three formulations to rats. A significant difference was observed in the main pharmacokinetic parameters between SMEDDS and the suspension, and a 3.25‐ and 2.97‐fold increase in the relative bioavailability of l‐THP and l‐ICP, respectively, was observed with the SMEDDS compared with the suspension formulation. It was concluded that SMEDDS enhanced the absorption of l‐THP and l‐ICP and delayed their release in brain.

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Development of solidified self-microemulsifying drug delivery systems containing l-tetrahydropalmatine: Design of experiment approach and bioavailability comparison

Cited by 45 publications

References 34 publications

Role of Hydrophilic Surfactants in the Emulsification Mechanistics of Type Iii Self-Micro-Emulsifying Drug Delivery Systems (Smedds)

Role of Hydrophilic Surfactants in the Emulsification Mechanistics of Type Iii Self-Micro-Emulsifying Drug Delivery Systems (Smedds)

Review of formulation and evaluation of self-micro emulsifying drug delivery system (SMEDDS)

Pharmacokinetic study of three different formulations of l‐tetrahydropalmatine in brain tissues of rats

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