Evaluation of Surfactant Effect on Self Micro Emulsifying Drug Delivery System (SMEDDS) of Lercanidipine Hydrochloride: Formulation and Evaluation

Akula, Samatha; Gurram, Aravind Kumar; Devireddy, Srinivas Reddy; Deshpande, Praful Balavant

doi:10.1007/s12247-015-9233-6

Cited by 14 publications

(4 citation statements)

References 39 publications

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“…Optimized formulations were analysed for stability using the standard centrifuge and freeze-thaw test. 26 Through the centrifuge test, formulations were centrifuged (Rotofix 32, Hettich Zentrifugen, Germany) for 30 minutes at 10 000 rpm, then were visually observed for alteration of visual appearance like phase separation, sedimentation, creaming, and cracking. If the formulations passed this test, they were subjected to freeze-thaw cycles.…”

Section: Methodsmentioning

confidence: 99%

“…54 Loading the lercanidipine hydrochloride in SMEDDS comprised of capmul MCM C8, brij35, cremophor EL, and propylene glycol created improved dissolution and permeation of the drug. 26 A c c e p t e d M a n u s c r i p t Furthermore, another study reported an improved bioavailability and dissolution for CoQ10 loaded in a SNEDDS system. 23 Other methods have also been used to evaluate drug-loaded SMEDDS.…”

Section: In Situ Intestinal Permeability: Single-pass Intestinal Perf...mentioning

confidence: 99%

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Optimization of a Self-microemulsifying Drug Delivery System for Oral Administration of the Lipophilic Drug, Resveratrol: Enhanced Intestinal Permeability in Rat

2022

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Purpose: This study aimed to formulate Resveratrol, a practically water-insoluble antioxidant in a self-microemulsifying drug delivery system (SMEDDS) to improve the solubility, release rate, and intestinal permeability of the drug. Methods: The suitable oil, surfactant, and co-surfactant were chosen according to the drug solubility study. Utilizing the design of experiment (DoE) method, the pseudo-ternary phase diagram was plotted based on the droplet size. In vitro dissolution study and the single-pass intestinal perfusion were performed for the investigation of in vitro and in-situ permeability for drugs formulated as SMEDDS in rat intestine using High-Performance Liquid Chromatography. Results: Castor oil, Cremophor RH60, and PEG 1500 were selected as oil, surfactant, and co-surfactant. According to the pseudo-ternary phase diagram, nine formulations developed microemulsions with sizes ranging between 145-967 nm. Formulations passed the centrifuge and freeze-thaw stability tests. The optimum formulation possessed an almost 2.5-fold higher cumulative percentage of in vitro released resveratrol, in comparison to resveratrol aqueous suspension within 120 minutes. The results of the in-situ permeability study suggested a 2.6-fold higher intestinal permeability for optimum formulation than that of the resveratrol suspension. Conclusions: SMEDDS can be considered suitable for the oral delivery of resveratrol according to the observed increased intestinal permeability, which could consequently enhance the bioavailability and therapeutic efficacy of the drug.

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Section: Methodsmentioning

confidence: 99%

Section: In Situ Intestinal Permeability: Single-pass Intestinal Perf...mentioning

confidence: 99%

Optimization of a Self-microemulsifying Drug Delivery System for Oral Administration of the Lipophilic Drug, Resveratrol: Enhanced Intestinal Permeability in Rat

2022

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“…The PDI values of liposomes were measured lower than 0.3. This PDI value is attributed to the uniformity in the droplet size distribution of formulations [12,13]. After binding of pDNA, the sizes and the PDI values of formulations have increased except for the formulation Lipo-2E:pDNA.…”

Section: Formation and Characterization Of Liposomesmentioning

confidence: 99%

A comparative study of cationic liposomes for gene delivery

Akbaba¹,

Akbaba²

2021

jrp

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In the field of gene delivery, non-viral vectors have become more attractive carriers for nucleic acids since they can overcome the significant drawbacks of viral systems such as safety, immunogenicity, and oncogenicity. Among non-viral vectors, cationic liposome-mediated gene delivery gives promising results for gene therapy approaches. This study aimed to develop cationic liposomes and examine the effectiveness in terms of gene delivery. For this purpose, cholesterol, lecithin, and cationic lipid containing liposomes have been developed by film hydration method. Two different cationic lipids, DDAB and EQ, and their different mole ratios were investigated. Characterization studies showed that obtained liposomes have appropriate physiochemical characteristics (~100 nm, homogenous in size and positive zeta potential) for gene delivery. Gel retardation assay revealed that they have DNA binding and protection ability against nucleases. According to the cytotoxicity evaluation performed on L929 cell line, EQ containing liposomes shows significantly less toxicity comparing DDAB containing liposomes (p<0.05). Furthermore, in vitro transfection study revealed that increasing the EQ mole ratio has increased transfection ability. The stability results showed that the optimal liposome which contains EQ in a higher mole ratio is stable during 90 days at 4 o C. Based on these findings, we propose that the developed optimal liposome system in this study could be considered as a suitable nucleic acid delivery vehicle base for gene therapy.

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“…Lately, SPNMS have demonstrated considerable potential to enhance the oral bioavailability of anticancer bioactives owing to their ability to circumvent the major hiccups faced by the latter [ 24 – 26 ]. Composed of lipidic constituents, water-insoluble (with HLB < 12; used in 0–20 parts) and water-soluble (with HLB > 12; used in 30–80 parts) emulgents, coemulgents, and cosolvents, these systems are known to produce ultrafine micelles (i.e., < 50 nm in size) in the gastrointestinal (GI) fluids [ 27 ]. Hence, SPNMS have been considered as one of the most promising technologies for a vast diversity of drugs [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems

Khurana

Gaspar

Welsby

et al. 2018

Drug Deliv. and Transl. Res.

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The current research work encompasses the development, characterization, and evaluation of self-assembled phospholipidic nano-mixed miceller system (SPNMS) of a poorly soluble BCS Class IV xanthone bioactive, mangiferin (Mgf) functionalized with co-delivery of vitamin E TPGS. Systematic optimization using I-optimal design yielded self-assembled phospholipidic nano-micelles with a particle size of < 60 nm and > 80% of drug release in 15 min. The cytotoxicity and cellular uptake studies performed using MCF-7 and MDA-MB-231 cell lines demonstrated greater kill and faster cellular uptake. The ex vivo intestinal permeability revealed higher lymphatic uptake, while in situ perfusion and in vivo pharmacokinetic studies indicated nearly 6.6- and 3.0-folds augmentation in permeability and bioavailability of Mgf. In a nutshell, vitamin E functionalized SPNMS of Mgf improved the biopharmaceutical performance of Mgf in rats for enhanced anticancer potency.Electronic supplementary materialThe online version of this article (10.1007/s13346-018-0498-4) contains supplementary material, which is available to authorized users.

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Evaluation of Surfactant Effect on Self Micro Emulsifying Drug Delivery System (SMEDDS) of Lercanidipine Hydrochloride: Formulation and Evaluation

Cited by 14 publications

References 39 publications

Optimization of a Self-microemulsifying Drug Delivery System for Oral Administration of the Lipophilic Drug, Resveratrol: Enhanced Intestinal Permeability in Rat

Optimization of a Self-microemulsifying Drug Delivery System for Oral Administration of the Lipophilic Drug, Resveratrol: Enhanced Intestinal Permeability in Rat

A comparative study of cationic liposomes for gene delivery

Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems

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