Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: Preparation and characterization

Liu, Jie; Gong, Tao; Wang, Chang-Guang; Zhong, Zhaohui; Zhang, Zhirong

doi:10.1016/j.ijpharm.2007.03.009

Cited by 233 publications

(119 citation statements)

References 37 publications

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“…These data of burst effect in SLNs were supported by the results reported in the literature (Rahman et al, 2010). The biphasic drug release pattern is very common with SLNs (Liu et al, 2007).…”

Section: In Vitro Release Studiessupporting

confidence: 85%

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Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Ansari¹,

Anwer²,

Jamil³

et al. 2015

Drug Delivery

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Objective: Insulin is a hormone used in the treatment of diabetes mellitus. Multiple injections of insulin every day may causes pain, allergic reactions at injection site, which lead to low patient compliance. The aim of this work was to develop and evaluate an efficient solid lipid nanoparticle (SLN) carrier for oral delivery of insulin. Methods: SLNs were prepared by double emulsion solvent evaporation (w/o/w) technique, employing glyceryltrimyristate (Dynasan 114) as lipid phase and soy lecithin and polyvinyl alcohol as primary and secondary emulsifier, respectively, and evaluated in vitro for particle size, polydispersity index (PDI) and drug entrapment. Results: Among the eight different developed formulae (F1-F8), F7 showed an average particle size (99 nm), PDI (0.021), high entrapment of drug (56.5%). The optimized formulation (F7) was further evaluated by FT-IR, DSC, XRD, in vitro release, permeation, stability, bioavailability and pharmacological studies. Insulin-loaded SLNs showed better protection from gastrointestinal environment as evident from the relative bioavailability, which was enhanced five times as compared to the insulin solution. A significant enhancement of relative bioavailability of insulin was observed, i.e. approximately five times of pure insulin solution when loaded in SLN (8.26% versus 1.7% only).

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Section: In Vitro Release Studiessupporting

confidence: 85%

“…Several studies of insulin-loaded solid lipid-based nanoparticles have recently been published however many of these either did not report bioavailability (Liu et al, 2007;Fonte et al, 2012) or reported pharmacological activity only (Sarmento et al, 2007;Zhang et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Ansari¹,

Anwer²,

Jamil³

et al. 2015

Drug Delivery

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“…Zhang et al (2013) reported that the incorporation of sodium cholate improved the intestinal absorption of candesartan from cilexetil-loaded lipid nanocarriers. Liu et al (2007) employed sodium cholate in solid lipid nanoparticles to improve the lipo-solubility of insulin. Zeng et al (2013) attempted to functionalize nanoparticles with cholic acid to improve docetaxel delivery to cervical cancer.…”

Section: Bile Salts In Drug Delivery Systemsmentioning

confidence: 99%

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Aburahma¹

2014

Drug Delivery

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Most of the new drugs, biological therapeutics (proteins/peptides) and vaccines have poor performance after oral administration due to poor solubility or degradation in the gastrointestinal tract (GIT). Though, vesicular carriers exemplified by liposomes or niosomes can protect the entrapped agent to a certain extent from degradation. Nevertheless, the harsh GIT environment exemplified by low pH, presence of bile salts and enzymes limits their capabilities by destabilizing them. In response to that, more resistant bile salts-containing vesicles (BS-vesicles) were developed by inclusion of bile salts into lipid bilayers constructs. The effectiveness of orally administrated BS-vesicles in improving the performance of vesicles has been demonstrated in researches. Yet, these attempts did not gain considerable attention. This is the first review that provides a comprehensive overview of utilizing BS-vesicles as a promising pharmaceutical carrier with a special focus on their successful applications in oral delivery of therapeutic macromolecules and vaccines. Insights on the possible mechanisms by which BSvesicles improve the oral bioavailability of the encapsulated drug or immunological response of entrapped vaccine are explained. In addition, methods adopted to prepare and characterize BSvesicles are described. Finally, the gap in the scientific researches tackling BS-vesicles that needs to be addressed is highlighted.

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“…Generally speaking, the particles were stable when the absolute value of the zeta potential was above 30 mV due to the electric repulsion between particles [26][27][28] . The average zeta potential of the SLB-PPC-SDC-MMs was (-39±5.0) mV, which suggests that the MMs obtained in this study could be a dynamic stable system.…”

Section: Zeta Potentialmentioning

confidence: 99%

Mixed micelles loaded with silybin-polyene phosphatidylcholine complex improve drug solubility

et al. 2010

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Aim: To prepare a novel formulation of phosphatidylcholine (PC)-bile salts (BS)-mixed micelles (MMs) loaded with silybin (SLB)-PC complex for parenteral applications. Methods: SLB-PC-BS-MMs were prepared using the co-precipitation method. Differential scanning calorimetry (DSC) analysis was used to confirm the formation of the complex and several parameters were optimized to obtain a high quality formulation. The water-solubility, drug loading, particle size, zeta potential, morphology and in vivo properties of the SLB-PC-BS-MMs were determined. Results: The solubility of SLB in water was increased from 40.83±1.18 µg/mL to 10.14±0.36 mg/mL with a high drug loading (DL) of 14.43%±0.44% under optimized conditions. The SLB-PC-BS-MMs were observed by transmission electron microscopy (TEM) and scanning electron microscopy (SEM) and showed spherical shapes. The particle size and zeta potential, as measured by photon correlation spectroscopy (PCS), were about 30±4.8 nm and -39±5.0 mV, respectively. In vivo studies showed that incorporation of the SLB-PC complex into PC-BS-MMs led to a prolonged circulation time of the drug. Conclusion:This novel formulation appears to be a good candidate for drug substances that exhibit poor solubility for parenteral administration.

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Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: Preparation and characterization

Cited by 233 publications

References 37 publications

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

Mixed micelles loaded with silybin-polyene phosphatidylcholine complex improve drug solubility

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