Tadalafil-loaded nanostructured lipid carriers using permeation enhancers

Baek, Jong-Suep; Pham, Cuong; Myung, Chang‐Seon; Cho, Cheong-Weon

doi:10.1016/j.ijpharm.2015.09.054

Cited by 54 publications

(22 citation statements)

References 47 publications

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“…In another study, the PS of SLNs decreased considerably from 426 to 311 nm and PDI reduced from 0.38 to 0.24 when soya lecithin concentration was increased from 20 to 50% [ 160 ]. Similar results have been reported for oleic acid [ 42 , 181 ], MCT [ 4 ], and phosphatidylcholine [ 169 ]. The smaller PS and PDI of NLCs produced at higher liquid lipid levels are attributed to reductions in lipid blend viscosity [ 4 , 42 , 182 ].…”

Section: Effect Of Formulation Parameters On Slns and Nlcs Producesupporting

confidence: 88%

Preparation of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Drug Delivery and the Effects of Preparation Parameters of Solvent Injection Method

2020

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Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have emerged as potential drug delivery systems for various applications that are produced from physiological, biodegradable, and biocompatible lipids. The methods used to produce SLNs and NLCs have been well investigated and reviewed, but solvent injection method provides an alternative means of preparing these drug carriers. The advantages of solvent injection method include a fast production process, easiness of handling, and applicability in many laboratories without requirement of complicated instruments. The effects of formulations and process parameters of this method on the characteristics of the produced SLNs and NLCs have been investigated in several studies. This review describes the methods currently used to prepare SLNs and NLCs with focus on solvent injection method. We summarize recent development in SLNs and NLCs production using this technique. In addition, the effects of solvent injection process parameters on SLNs and NLCs characteristics are discussed.

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Section: Effect Of Formulation Parameters On Slns and Nlcs Producesupporting

confidence: 88%

Preparation of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Drug Delivery and the Effects of Preparation Parameters of Solvent Injection Method

2020

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“…The partition coefficient and solubility of PR in the lipid matrix are major factors determining encapsulation efficiency (EE) and loading capacity (LC) in the NLCs [ 11 ]. Therefore, we investigated the partition coefficient of PR in solid lipids and the solubility of PR in liquid lipids to determine conditions for loading the maximum amount of PR into the NLC.…”

Section: Resultsmentioning

confidence: 99%

The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers

Kim

Choi

et al. 2017

Nanomaterials

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Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were prepared by the hot-melted ultrasonic method. Glycerol monostearate and olive oil were selected as the solid lipid and liquid lipid for considering the solubility of PR in liquid lipid and partition coefficient of PR in solid lipid, respectively. The particle size and polydispersity index of PR-NLCs were 57.9 ± 1.3 nm and 0.24 ± 0.01, respectively. The encapsulation efficiency and loading capacity of PR-NLCs were 93.1 ± 4.2% and 8.5 ± 0.4%, respectively. The stability test demonstrated that the incorporation of PR into NLCs conferred excellent physicochemical stability and photo stability for at least three months at 4 °C in the dark and 25 °C under daylight. In vitro release of PR-NLCs revealed a sustained release pattern. Cellular tyrosinase assay showed that PR-NLCs could significantly inhibit tyrosinase activity in melanoma cells, suggesting that NLCs can be used as a biocompatible nanocarrier for the effective delivery of skin whitening agents.

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“…However, suffering from poor aqueous solubility, tadalafil is a BCS class II drug. Numerous approaches for enhancing its dissolution rate were reported including the use of solid dispersions 29 , complexation with cyclodextrins 30 , inclusion in microporous silicas 31 , formulation of nanosuspensions 32 , use of self-nanoemulsifying drug delivery systems (SNEDDS) 33 , and nanostructured lipid carriers (NLCs) 34 . However, to the best of our knowledge, liquisolid technique has never been utilized to promote the dissolution of tadalafil in the reported literatures.…”

Section: Introductionmentioning

confidence: 99%

Dissolution enhancement of tadalafil by liquisolid technique

Xing

Yang

et al. 2016

Pharmaceutical Development and Technology

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This study aimed to enhance the dissolution of tadalafil, a poorly water-soluble drug by applying liquisolid technique. The effects of two critical formulation variables, namely drug concentration (17.5% and 35%, w/w) and excipients ratio (10, 15 and 20) on dissolution rates were investigated. Pre-compression tests, including particle size distribution, flowability determination, Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and scanning electron microscopy (SEM), were carried out to investigate the mechanism of dissolution enhancement. Tadalafil liquisolid tablets were prepared and their quality control tests, dissolution study, contact angle measurement, Raman mapping, and storage stability test were performed. The results suggested that all the liquisolid tablets exhibited significantly higher dissolution rates than the conventional tablets and pure tadalafil. FT-IR spectrum reflected no drug-excipient interactions. DSC and XRD studies indicated reduction in crystallinity of tadalafil, which was further confirmed by SEM and Raman mapping outcomes. The contact angle measurement demonstrated obvious increase in wetting property. Taken together, the reduction of particle size and crystallinity, and the improvement of wettability were the main mechanisms for the enhanced dissolution rate. No significant changes were observed in drug crystallinity and dissolution behavior after storage based on XRD, SEM and dissolution results.

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Tadalafil-loaded nanostructured lipid carriers using permeation enhancers

Cited by 54 publications

References 47 publications

Preparation of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Drug Delivery and the Effects of Preparation Parameters of Solvent Injection Method

Preparation of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Drug Delivery and the Effects of Preparation Parameters of Solvent Injection Method

The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers

Dissolution enhancement of tadalafil by liquisolid technique

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