Improvement of bioavailability and photostability of amlodipine using redispersible dry emulsion

Jang, Dong‐Jin; Jeong, Eun Ju; Lee, Hwa-Mi; Kim, Bae-Chan; Lim, Soo-Jeong; Kim, Chong‐Kook

doi:10.1016/j.ejps.2006.04.013

Cited by 85 publications

(50 citation statements)

References 23 publications

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“…Jang D-J et al enhanced the stability of amlodipine against photodegradation by formulating dry emulsion. Also, there self nanoemulsifying oily formulation (SNEOFs) was 2.9 times enhancement of bioavailability of the formulation of amlodipine (Jang D-J et al, 2006).…”

Section: Lipid-based Nanoparticlesmentioning

confidence: 99%

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Nanocarriers as treatment modalities for hypertension

et al. 2017

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Hypertension, a worldwide epidemic at present, is not a disease in itself rather it is an important risk factor for serious cardiovascular disorders including myocardial infarction, stroke, heart failure, and peripheral artery disease. Though numerous drugs acting via different mechanism of action are available in the market as conventional formulations for the treatment of hypertension but they face substantial challenges regarding their bioavailability, dosing and associated adverse effects which greatly limit their therapeutic efficacies. Various studies have demonstrated that nanocarriers can significantly increase the drug bioavailability thereby reducing the frequency of dosing in addition to minimizing toxicity associated with high dose of the drug. The present review provides an insight into the challenges associated with the conventional antihypertensive formulations and need for oral nanoparticulate systems in order to overcome problems associated with conventional formulations. Hypertension has circadian pattern of blood pressure, therefore chronotherapeutics can play a decisive role for the treatment, and however, nanoparticulate system can play major role in hypertension management. Future prospective for particulate nanocarriers in drug delivery for hypertension includes chronotherapeutics and emerging technique like gene therapy which is also covered in the review.

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Section: Lipid-based Nanoparticlesmentioning

confidence: 99%

“…Both drugs were delivered by utilizing nanoemulsion as a drug delivery system. Their pharmacokinetic data revealed the stability and enhanced bioavailability (Jang D-J et al, 2006;Havanoor et al, 2014). Chronotherapeutics can deliver drugs at the time when symptoms occur like during night and early morning as in the case with hypertension.…”

Section: Introductionmentioning

confidence: 99%

Nanocarriers as treatment modalities for hypertension

et al. 2017

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“…By looking at the ranges of pre-compression parameters, all the formulations F1 to F12 had excellent to pair to flow properties. The results of pre-formulation parameters of all formulations were in the acceptable range as per the specifications [6,7,23]. Hence, we were preceded by further studies.…”

Section: Evaluation Of Pre-compression Parameters Of Formulation Blendmentioning

confidence: 99%

“…The bioavailability of these drugs can be limited by poor dissolution of the drug into aqueous bodily fluids the following administration. This rate-limiting step may, therefore, be critical to rapidly attaining therapeutically effective amlodipine and atorvastatin drugs levels, inadequate and variable bioavailability and gastrointestinal mucosal toxicity [6][7][8][9][10]. A number of novel approaches for enhancing the low aqueous solubility of drugs have been attempted and continued to evolve over a period.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Tablet Prepared by Coamorphous System Containing Anti-Hypertensive and Anti-Hyperlipidemic Drug

Adahalli

Talluri

2016

Int J Pharm Pharm Sci

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Objective: Amlodipine besylate (AML) and Atorvastatin calcium (ATR) belong to biopharmaceutical classification system (BCS) class II (i.e. low solubility and high permeability) which leads to variable bioavailability. Hence, the aim of this study was to enhance the solubility of both drugs by utilizing the co-amorphous technique. This converted form and physical mixture of both drugs were utilized in the formulation of tablets. Methods:The co-amorphous system was prepared by using rotary flash evaporator. Solubility study was carried out to investigate the dissolution advantage of prepared co-amorphous form. Total twelve formulations were formulated by keeping constant drugs concentrations utilizing direct compression technique among which F1 to F6 contains co-amorphous AML-ATR (Co-A AML-ATR) and F7 to F12 contains a physical mixture of AML and ATR as active pharmaceutical ingredient (APIs). Pre-compression and post-compression studies were carried out to all twelve formulations. Stability study was performed to the optimized formulations as per ICH guidelines.Results: Mixture obtained after evaporation was found to become amorphous. FTIR study shows no evidence of intermolecular interactions between AML and ATR. The solubility of both AML and ATR were increased in almost one fold as compared to their respective crystalline counterparts. Pre-compression parameters of all twelve formulations blend fall under excellent to fair to flow properties. Post-compression parameters of all twelve formulations were within the specifications. But in vitro drug release of formulations F5, F6, F11, and F12 showed % drug release as per IP. Stability study of optimized formulations was observed with, no significant difference in % drug release. Conclusion:The co-amorphous system can be prepared by utilizing rotary flash evaporator and the same was confirmed by XRPD and FTIR studies. The dissolution rate of the co-amorphous system was greater than that of the crystalline counterpart. Based on the results; F5 and F6 are considered as optimized formulations. Optimized formulations were stable during the stability study.

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“…10,11 In order to address these drawbacks, formulation approaches using solid dispersion, 12 liposomes, 13 cyclodextrin complexes, 14,15 and nanoparticles have been reported. [16][17][18] Although some progress has been achieved, these approaches have issues of poor drug loading, drug leakage, burst release patterns, and poor physicochemical stability that are unaddressed.…”

Section: Introductionmentioning

confidence: 99%

Entrapment of curcumin into monoolein-based liquid crystalline nanoparticle dispersion for enhancement of stability and anticancer activity

Baskaran¹,

Madheswaran²,

Sundaramoorthy³

et al. 2014

IJN

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Despite the promising anticancer potential of curcumin, its therapeutic application has been limited, owing to its poor solubility, bioavailability, and chemical fragility. Therefore, various formulation approaches have been attempted to address these problems. In this study, we entrapped curcumin into monoolein (MO)-based liquid crystalline nanoparticles (LCNs) and evaluated the physicochemical properties and anticancer activity of the LCN dispersion. The results revealed that particles in the curcumin-loaded LCN dispersion were discrete and monodispersed, and that the entrapment efficiency was almost 100%. The stability of curcumin in the dispersion was surprisingly enhanced (about 75% of the curcumin survived after 45 days of storage at 40°C), and the in vitro release of curcumin was sustained (10% or less over 15 days). Fluorescence-activated cell sorting (FACS) analysis using a human colon cancer cell line (HCT116) exhibited 99.1% fluorescence gating for 5 μM curcumin-loaded LCN dispersion compared to 1.36% for the same concentration of the drug in dimethyl sulfoxide (DMSO), indicating markedly enhanced cellular uptake. Consistent with the enhanced cellular uptake of curcumin-loaded LCNs, anticancer activity and cell cycle studies demonstrated apoptosis induction when the cells were treated with the LCN dispersion; however, there was neither noticeable cell death nor significant changes in the cell cycle for the same concentration of the drug in DMSO. In conclusion, entrapping curcumin into MO-based LCNs may provide, in the future, a strategy for overcoming the hurdles associated with both the stability and cellular uptake issues of the drug in the treatment of various cancers.

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Improvement of bioavailability and photostability of amlodipine using redispersible dry emulsion

Cited by 85 publications

References 23 publications

Nanocarriers as treatment modalities for hypertension

Nanocarriers as treatment modalities for hypertension

Formulation and Evaluation of Tablet Prepared by Coamorphous System Containing Anti-Hypertensive and Anti-Hyperlipidemic Drug

Entrapment of curcumin into monoolein-based liquid crystalline nanoparticle dispersion for enhancement of stability and anticancer activity

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