Design and Evaluation of a Self-Emulsifying Drug Delivery System of Aripiprazole

Ramya, A. R.; Sudheer, Preethi; Mohameid, A. S.; Das, Asha

doi:10.36468/pharmaceutical-sciences.607

Cited by 10 publications

(5 citation statements)

References 13 publications

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“…Isopropyl myristate is the ester of isopropyl alcohol and myristic acid. It has usually been used for topical pharmaceutical preparations, but oral application in the preparation of SMEDDS or microemulsions has also been reported [ 54 , 55 , 56 ].…”

Section: Discussionmentioning

confidence: 99%

Microemulsions Enhance the In Vitro Antioxidant Activity of Oleanolic Acid in RAW 264.7 Cells

Stefani

Vasarri²,

Salvatici³

et al. 2022

Pharmaceutics

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Oleanolic acid (OA) is the main triterpenic acid of olive leaves known for numerous pharmacological properties, including antioxidant activity. However, it is poorly soluble in water and consequently with low bioavailability, which limits its pharmacological application. Microemulsions (MEs) are dispersed systems consisting of two immiscible phases that promote rapid solubilization and absorption in the gastrointestinal tract. To improve both solubility and intestinal permeability of this molecule, OA has been formulated in two different microemulsions (ME-1 and ME-2). A solubility screening was carried out to select the ME components, and pseudoternary phase diagrams were constructed to evaluate the region of existence and select the appropriate amount of the constituents. ME-1 was prepared using Capmul PG-8/NF as the oily phase, and Transcutol and Tween 20 (7:3) as surfactants, while ME-2 contained Nigella oil and Isopropil myristate as the oily phase, and Transcutol HP and Cremophor EL (2:1) as surfactants. The OA solubility was increased by 1000-fold and 3000-fold in ME-1-OA and ME-2-OA, respectively. The MEs’ droplet size and the PdI were evaluated, and the stability was assessed for 8 weeks by monitoring chemical and physical parameters. The parallel artificial membrane permeability assay (PAMPA) also demonstrated an enhanced intestinal permeability of both OA formulations compared with free OA. The potential ability of both MEs to enhance the bioactivity of OA against LPS-induced oxidative stress in RAW 264.7 murine macrophages was also investigated. Overall, this study suggests that both MEs promote a bio-enhancement of the protective action of OA against the LPS-induced pro-oxidant stress in macrophages. Overall, this study suggests that MEs could be an interesting formulation to improve OA oral bioavailability with potential clinical applications.

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Section: Discussionmentioning

confidence: 99%

Microemulsions Enhance the In Vitro Antioxidant Activity of Oleanolic Acid in RAW 264.7 Cells

Stefani

Vasarri²,

Salvatici³

et al. 2022

Pharmaceutics

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“…In Biopharmaceutical classification system (BCS), APZ had low solubility and low permeability [7]. APZ is soluble in organic solvents such as ethanol, DMSO Sulphoxide), and Dimethyl Formamide (DMF) which should be purged with an inert gas.…”

Section: Properties Of Apzmentioning

confidence: 99%

“…This review has become needful in view of the rapid progress in APZ development, its assay in both bulk and pharmaceutical dosage forms as well as their determination in biological fluids. (5) electrochemical techniques; (6) XRD; (7) have been analyzed by various methods which have been described in different literatures. Among the reported analytical methods, HPLC was found to be the most developed and validated method for the , followed by other methods This review has become needful in view research and development, its assay in both bulk and pharmaceutical dosage forms as well as their…”

Section: Analytical Status Of Apzmentioning

confidence: 99%

A Compact Analytical Profile of Aripiprazole: Analytical Methodologies

Athira¹,

Rishad²,

Babu

et al. 2021

JPRI

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Aripiprazole (APZ) is an antipsychotic drug that belongs to benzisoxazole derivatives and is used to treat schizophrenia as well as acute manic or mixed effects in patients with bipolar 1 disorder. APZ is used to treat certain mental, mood disorders such as bipolar disorder, Schizophrenia, Tourette's syndrome, and irritability associated with autistic disorder. It may also be used in combination with other medication to treat depression. The present review article would be useful for prospective studies for researchers interested in APZ formulation production and quality management. Using a thorough computer assisted literature survey; this review touches upon the various reported analytical methods for the quantification of APZ both in API (Active Pharmaceutical Ingredient) and pharmaceutical dosage forms. The present write-up also encompasses the various published research articles like Spectroscopy techniques, X- Ray Diffraction (XRD), Electro Chemical Technique, Differential Scanning Calorimeter (DSC) and Capillary Electrophoresis. This is the first review article in this series with focus on the analytical profile of APZ. Although, several methods were reported in the literature, HPLC stands out first for the quantification of APZ.

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“…The various technique is utilized to enhance oral bioavailability of the poorly water-soluble drug, the oral route has been the ideal route of drug administration for the endless treatment of diseases as it offers more patient compliance [1]. 40 % of new drug applicants show low solvency in water, which is a test being developed of the ideal oral solid dosage form as far as formulation development and bioavailability of new pharmaceutical preparation [1,2]. Various strategies are used for improving the bioavailability of those medications like the salt arrangement, pH change, βcyclodextrin complex, microemulsion, and so forth [3].…”

Section: Introductionmentioning

confidence: 99%

“…SMEDDS are class of emulsion that has gotten specific consider-ation as a method for upgrading oral bioavailability of poor soluble drugs [4]. SMEDDS or self-emulsifying oil formulations (SEOF) are characterized as isotropic blends of natural and synthetic oils, delete these words, surfactants, or then again, at least one hydrophilic solvents and cosolvents/surfactants [2,3]. SEDDS ordinarily produce emulsions with a globule size somewhere in the range of 100 and 300 nm while SMEDDS can have droplet size somewhere near 50 nm [3,5].…”

Section: Introductionmentioning

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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Design and Evaluation of a Self-Emulsifying Drug Delivery System of Aripiprazole

Cited by 10 publications

References 13 publications

Microemulsions Enhance the In Vitro Antioxidant Activity of Oleanolic Acid in RAW 264.7 Cells

Microemulsions Enhance the In Vitro Antioxidant Activity of Oleanolic Acid in RAW 264.7 Cells

A Compact Analytical Profile of Aripiprazole: Analytical Methodologies

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

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