Preparation and stabilization of nifedipine lipid nanoparticles

Kamiya, Seitaro; Yamada, Mariko; Kurita, Takurou; Miyagishima, Atsuo; Arakawa, Masayuki; Sonobe, Takashi

doi:10.1016/j.ijpharm.2007.10.049

Cited by 28 publications

(21 citation statements)

References 24 publications

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“…The mean particle size and zeta potential of the nanoparticles were about 55 nm and −61.8 mV, respectively, and both remained constant over 4 months below 6°C in the dark conditions, suggesting that the negative charge of the phospholipid, dipalmitoyl phosphatidylglycerol, was effective in preventing coagulation of the particles. The particles could be freeze-dried after addition of sugars (glucose, fructose, maltose or sucrose) and exhibited excellent solubility (36).…”

Section: Solid Lipid-based Systemsmentioning

confidence: 99%

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Kromp²,

et al. 2010

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Phospholipids become increasingly important as formulation excipients and as active ingredients per se. The present article summarizes particular features of commonly used phospholipids and their application spectrum within oral drug formulation and elucidates current strategies to improve bioavailability and disposition of orally administered drugs. Advantages of phospholipids formulations not only comprise enhanced bioavailability of drugs with low aqueous solubility or low membrane penetration potential, but also improvement or alteration of uptake and release of drugs, protection of sensitive active agents from degradation in the gastrointestinal tract, reduction of gastrointestinal side effects of non-steroidal anti-inflammatory drugs and even masking of bitter taste of orally applied drugs. Technological strategies to achieve these effects are highly diverse and offer various possibilities of liquid, semi-liquid and solid lipid-based formulations for drug delivery optimization.

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Section: Solid Lipid-based Systemsmentioning

confidence: 99%

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Kromp²,

et al. 2010

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“…NI-lipid nanoparticle suspensions were prepared as described previously (Kamiya et al, 2008). Briefly, 20 or 40 mg of NI and 1000 mg of lipid (HSPC:DPPG = 5:1 molar ratio) were added to a mortar, and physically mixed.…”

Section: Preparation Of Ni-lipid Nanoparticle Suspensionsmentioning

confidence: 99%

“…Recently, using the combination of co-grinding by a roll milling and subsequent high-pressure homogenization, we succeeded in preparing nifedipine (NI), a poorly water-soluble compound, -lipid nanoparticle suspensions without any organic solvent at any stage of the process (Kamiya et al, 2008). The study showed that the mean particle size of the NI-lipid nanoparticle suspensions was about 55 nm, and incorporation of gelatin to the nanoparticle suspensions allowed reproduction of the nano-particle size after reconstitution with water up to 24 h storage at 6 • C. However, it was difficult to maintain the mean particle size of the NI-lipid nanoparticles for a longer time.…”

Section: Introductionmentioning

confidence: 99%

Freeze-dried nifedipine-lipid nanoparticles with long-term nano-dispersion stability after reconstitution

Ohshima

Miyagishima

Kurita

et al. 2009

International Journal of Pharmaceutics

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“…[1][2][3] Recently, we successfully prepared lipid nanoparticles (LNs), which had a mean particle size of approximately 50 nm with a narrow particle size distribution, using wet milling, roll mixing, and high pressure homogenization to form small particles. 4) The LNs improved the solubility of nifedipine (NI), a poorly water-soluble drug, and improved its oral absorption of NI when NI-LNs were administrated to rats. 5) NI-LNs showed excellent long-term stability in suspension for approximately 4 months in cool and dark conditions, and freeze-drying techniques combined with sugar as a cryoprotectant allowed the preparation of LNs with a good aqueous re-dispersibility.…”

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confidence: 99%

Effect of Alkyl Chain Length and Unsaturation of the Phospholipid on the Physicochemical Properties of Lipid Nanoparticles

Funakoshi

Iwao

Noguchi

et al. 2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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Previously, we developed lipid nanoparticles (LNs) containing poorly water-soluble drugs using two types of phospholipids, a neutral phospholipid (hydrogenated soybean phosphatidylcholine) and a negativelycharged phospholipid (dipalmitoylphosphatidylglycerol), with mean particle sizes of less than 100 nm. Here, we studied the effects of alkyl chain length and unsaturation of neutral and negatively-charged phospholipids on the physicochemical properties of LNs. Three neutral phospholipids, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine, having different alkyl chain lengths, were compared. The mean particle size of the LNs increased with the alkyl chain length, while the concentration of the drug entrapped in the LNs decreased. The particle size of all of the LNs could be maintained at less than 100 nm for 1 month in cool and dark conditions, with the LNs with longer alkyl chain lipids showing greater stability. In the unsaturated phospholipids, the double bond in the alkyl chain of dioleoylphosphatidylcholine and dierucoylphosphatidylcholine did not affect the physicochemical properties of the LNs. The negatively-charged phospholipids dipalmitoylphosphatidylglycerol and distearoylphosphatidylglycerol were also compared; LNs with longer alkyl chain lipids had larger particle sizes and lower drug concentrations, similar to the results for neutral phospholipids. We concluded that although some changes in physicochemical properties were observed among LNs with different phospholipid alkyl chain lengths, this methodology was general. LNs with suitable physicochemical properties could be prepared irrespective of the type of phospholipids used.Key words lipid nanoparticle; poorly water-soluble drug; phospholipid; alkyl chain Many candidate active pharmaceutical ingredients (APIs) in formulations show poor solubility in water. To enhance the solubility of such poorly water-soluble APIs, the use of nanoparticle formulations with particle sizes less than 100 nm has recently attracted considerable attention in the field of pharmaceutical research.1-3) Recently, we successfully prepared lipid nanoparticles (LNs), which had a mean particle size of approximately 50 nm with a narrow particle size distribution, using wet milling, roll mixing, and high pressure homogenization to form small particles.4) The LNs improved the solubility of nifedipine (NI), a poorly water-soluble drug, and improved its oral absorption of NI when NI-LNs were administrated to rats. 5) NI-LNs showed excellent long-term stability in suspension for approximately 4 months in cool and dark conditions, and freeze-drying techniques combined with sugar as a cryoprotectant allowed the preparation of LNs with a good aqueous re-dispersibility.6,7) NI-LNs lyophilized with trehalose exhibited suitable pharmacokinetic properties and good biocompatibility. 8) Generally, two types of phospholipids, neutral phosphatidylcholine (PC) and negatively-charged phosphatidylglycerol (PG) are used to prepare LNs. PG was added to...

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Preparation and stabilization of nifedipine lipid nanoparticles

Cited by 28 publications

References 24 publications

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Freeze-dried nifedipine-lipid nanoparticles with long-term nano-dispersion stability after reconstitution

Effect of Alkyl Chain Length and Unsaturation of the Phospholipid on the Physicochemical Properties of Lipid Nanoparticles

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