Formulation and in Vivo Evaluation of Self-Nanoemulsifying Drug Delivery System of Ramipril in Wistar Rats

Jayapal, Nallapu; Vishnu, Y Vamshi

doi:10.22159/ajpcr.2021.v14i7.42003

Cited by 4 publications

(2 citation statements)

References 14 publications

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“…SNEDDS has also shown to be effective in enhancing the bioavailability of drugs that are sensitive to enzymatic degradation. With its potential to improve drug efficacy and patient compliance, SNEDDS is a promising tool for developing novel drug delivery systems [14][15][16].…”

Section: Fig 3: Format Of Liposome Imagingmentioning

confidence: 99%

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

AL-SHOUBKI,

H. TEAIMA,

ABDELMONEM

et al. 2023

Int J App Pharm

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This review article discusses Rivaroxaban (RXB), an anticoagulant that has gained much attention due to its ability to prevent blood clots from forming in the body. However, one of the major challenges pharmaceutical companies face is the low water solubility of RXB, which can lead to difficulties in formulating the drug for oral administration and affect the drug's bioavailability. However, to the best of our knowledge, limited studies have explored enhancing the bioavailability of the RXB. Most of these studies have been purely academic and impractical for industrial use. Therefore, this review article aims to discuss successful studies that have increased the bioavailability of RXB. The goal is to inspire researchers to develop this new drug further. The article covers seven strategies for enhancing the bioavailability of RXB, including microspheres, liposomes, self-nano emulsifying drug delivery system, solid lipid nanoparticles, cocrystals, sustained release, and solid dispersion. The studies discussed in this review offer valuable insights into developing novel drug delivery systems that can help overcome the limitations of existing drugs.

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Section: Fig 3: Format Of Liposome Imagingmentioning

confidence: 99%

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

AL-SHOUBKI,

H. TEAIMA,

ABDELMONEM

et al. 2023

Int J App Pharm

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“…Self-nanoemulsifying drug delivery systems (SNEDDS) is an effective, smart and more adequate formulation approach for poorly soluble drugs, compared to wide range of lipid-based systems. SNEDDS can enhance oral bioavailability by improving the drug solubility, dissolution behavior in GIT and gut permeability [5][6][7]. In addition, the drug loading capacity of conventional SNEDDS ranges only from 50-90% of the equilibrium solubility of drug and this result in more amount of formulation to reach the therapeutic level [8].…”

Section: Introductionmentioning

confidence: 99%

Formulation and in Vivo Evaluation of Pemigatinib Super Saturable Self-Nano Emulsifying Drug Delivery System

REDDY,

GUBBIYAPPA

2023

Int J App Pharm

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Objective: Pemigatinib is an active component in treatment of cholangiocarcinoma, but the low solubility and bioavailability of Pemigatinib limit its wide application. The aim of the present study was to prepare and evaluate supersaturable self-nanoemulsifying drug delivery systems (sSNEDDS) followed by investigating and comparing the pharmacokinetic profiles of Pemigatinib and Pemigatinib sSNEDDS in rat plasma by HPLC. Methods: Pemigatinib loaded SNEDDS were obtained by dissolving drug in the isotropic mixture of oil, surfactant, and co-surfactant. The conventional SNEDDS were converted to sSNEDDS by precipitation method by using an experimented polymer. An appropriate high sensitivity and selectivity was applied to the comparison of plasma pharmacokinetics in Pemigatinib and Pemigatinib sSNEDDS using Entrectinib as an internal standard (IS). Results: The droplet of sSNEDDS ranges from 166.78±3.14 to 178.86±1.24 nm with PDI 0.212–0.256, transmission electron microscopy images revealed the spherical shape of the nanodroplets, emulsification time was 15 secs when added to physiological fluids, percent transmittance of the diluted formulation was 99.12±0.46, and viscosity was 574±26 centipoises indicating the good flow ability. FTIR and DSC studies indicated the amorphization of the drug. The dissolution profile of sSNEDDS indicated the faster release of drug compared to both pure drug suspension and SNEDDS formulation. Cmax of the sSNEDDS 3.52±0.13ng/ml was significant (P<0.05) as compared to the pure drug suspension formulation 2.82±0.42 ng/ml. The AUC0-t, AUC0–∞ of sSNEDDS was increased, while the Tmax and t1/2 was decreased. Moreover, the AUC value in the sSNEDDS group was significantly increased and the relative bioavailability was calculated to be 69% when compared with that of the Pemigatinib group. Conclusion: These results concluded that Pemigatinib sSNEDDS when compared with pure drug after a single oral administration and the formulation modification of Pemigatinib into sSNEDDS can effectively enhance gastrointestinal absorption and relative bioavailability by improving solubility and dissolution rate.

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Development and validation of a stability indicating UPLC-DAD method coupled with MS-TQD for ramipril and thymoquinone in bioactive SNEDDS with in silico toxicity analysis of ramipril degradation products

Elzayat,

Sherif,

Shahba

et al. 2024

Open Chemistry

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The identification of degradation products of therapeutic molecules in pharmaceutical formulations has gained significant attention due to their potential impact on patient safety. Ramipril (RP), an antihypertensive agent, was incorporated into a self-nanoemulsifying drug delivery system (SNEDDS), which greatly enhanced its bioavailability. However, none of the previous studies have investigated the toxicological effects of these degradation products that may form during storage. Moreover, a bioactive SNEDDS containing black cumin oil (BCO) and its bioactive ingredient, thymoquinone (TQ), was used to further enhance the therapeutic activity of RP. To assess the stability of the proposed formulation, a validated ultrahigh-performance liquid chromatography (UPLC) method was developed to simultaneously measure the concentrations of RP and TQ. The formulation was subjected to accelerated stress conditions to facilitate drug degradation. The resulting degradation products were analyzed using mass spectroscopy (MS) to determine their molecular mass, and their chemical structures were in silico predicted using Zeneth Nexus software, while their toxicity was assessed using in silico Derek Nexus software. RP and TQ, along with their degradation products, were separated using an HSS T3 column at a flow rate of 0.25 mL/min. The detection wavelengths for RP and TQ were 210 and 254 nm, respectively. The developed UPLC method exhibited acceptable linearity for both RP and TQ, with correlation coefficient (r 2) values exceeding 0.9995 and 0.9998, respectively. The method provided accurate, precise, and high-resolution analysis of both drugs and their degradation products within a short run time of less than 3.2 min. The toxicity and mutagenicity of two alkaline degradation products of RP were predicted using in silico software Derek Nexus (version 6.3). Several toxicity endpoints, including chromosomal damage, skin sensitization, and hepatotoxicity, were predicted. Overall, the developed method can be used to evaluate the stability and integrity of RP and TQ during the development of the proposed antihypertensive formulation.

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Formulation and in Vivo Evaluation of Self-Nanoemulsifying Drug Delivery System of Ramipril in Wistar Rats

Cited by 4 publications

References 14 publications

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

Formulation and in Vivo Evaluation of Pemigatinib Super Saturable Self-Nano Emulsifying Drug Delivery System

Development and validation of a stability indicating UPLC-DAD method coupled with MS-TQD for ramipril and thymoquinone in bioactive SNEDDS with in silico toxicity analysis of ramipril degradation products

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