Nanostructured lipid carriers (NLC) based topical gel of flurbiprofen: Design, characterization and in vivo evaluation

Han, Fei; Yin, Ran; Che, Xin; Yuan, Jing; Cui, Yanan; Yin, He; Li, Sanming

doi:10.1016/j.ijpharm.2012.08.040

Cited by 95 publications

(22 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The introduction of fluid lipids still allows the lipid nanoparticles to remain in a solid state at room temperature, but the crystal lattice in the lipid particles becomes somewhat imperfect, improving both drug loading capacity and physical stability [26]. NLCs have been used as topical carrier for many drugs, such as acitretin, non-steroidal anti-inflammatory drugs (NSAIDs; ketoprofen, indomethacin), antioxidants (lutein, CoQ10), flubiprofen, clotrimazole, and celecoxib [27,28,29,30,31,32]. These encouraging results suggest that POD-loaded NLCs will exhibit enhanced therapeutic efficiency against CA.…”

Section: Introductionmentioning

confidence: 99%

Podophyllotoxin-Loaded Nanostructured Lipid Carriers for Skin Targeting: In Vitro and In Vivo Studies

et al. 2016

View full text Add to dashboard Cite

Nanostructured lipid carriers (NLC) exhibit high skin targeting efficiency and good safety. They are promising vehicles for topical drug delivery. This study aims to increase the skin distribution of podophyllotoxin (POD) by incorporating it into NLCs. Two kinds of POD-loaded NLCs (POD-NLCs)-POD-NLC formulation 1 and POD-NLC formulation 2 -were prepared and characterized. Their skin targeting efficiencies were compared by conducting in vitro and in vivo experiments. Obviously smaller mean particle size was observed for POD-NLC formulation 1 (106 nm) than POD-NLC formulation 2 (219 nm), whereas relatively low POD loadings (less than 0.5%) were observed for both POD-NLC formulation 1 (0.33%) and POD-NLC formulation 2 (0.49%). Significantly higher in vitro and in vivo rat skin deposit amounts of POD (p < 0.01) were detected after the topical application of POD-NLC formulation 1 compared to POD-NLC formulation 2 . To visualize the skin distribution behavior of hydrophobic active pharmaceutical ingredients (APIs) when NLCs were used as carriers, POD was replaced with Nile red (NR-a hydrophobic fluorescent probe), and the distribution behavior of NR-NLC formulation 1 and NR-NLC formulation 2 in rat skin in vivo was observed using confocal laser scanning microscopy (CLSM). Higher fluorescent intensity was observed in rat skin after the topical application of NR-NLC formulation 1 than NR-NLC formulation 2 , suggesting that higher skin targeting efficiency might be obtained when NLCs with smaller mean particle size were used as carriers for hydrophobic APIs. This result was in accordance with those of skin distribution evaluation experiments of POD-NLCs. Skin irritation property of POD-NLC formulation 1 was investigated and no irritation was observed in intact or damaged rabbit skin, suggesting it is safe for topical use. Our results validated the safety of NLCs when applied topically. More importantly, mean particle size might be an important parameter for formulation optimization when NLCs are used as carriers for hydrophobic APIs for topical application, considering that their loading is relatively low.

show abstract

Section: Introductionmentioning

confidence: 99%

Podophyllotoxin-Loaded Nanostructured Lipid Carriers for Skin Targeting: In Vitro and In Vivo Studies

et al. 2016

View full text Add to dashboard Cite

show abstract

“…In brief, Carbopol 934 P (1%) was dispersed in distilled water and allowed to hydrate for 4 to 5 h. Propylene glycol (10%) and glycerol (30%) were added subsequently to the aqueous dispersion, and 0.5 mL of triethanolamine was added under gentle stirring to avoid the inclusion of air. 23 Lyophilized MTXNLC powder equivalent to 600 mg of the drug was incorporated into the gel under gentle stirring. The dispersion was neutralized with 1% w/v NaOH to pH 6.0, and water (58.4%) was added to make up the final weight of gel up to 100%.…”

Section: Preparation Of Mtx Loaded Nlcs Gelmentioning

confidence: 99%

<p>Methotrexate-Loaded Nanostructured Lipid Carrier Gel Alleviates Imiquimod-Induced Psoriasis by Moderating Inflammation: Formulation, Optimization, Characterization, In-Vitro and In-Vivo Studies</p>

Agrawal

Mahajan

et al. 2020

IJN

View full text Add to dashboard Cite

Introduction: Methotrexate exhibits poor cutaneous bioavailability and systemic side effects on topical administration, so there is an unmet need for a novel carrier and its optimized therapy. Methotrexate-loaded nanostructured lipid carriers (MTXNLCs) were formulated and characterized to determine in vitro drug release and evaluate the role of MTXNLC gel in the topical treatment of psoriasis. Methods: A solvent diffusion technique was employed to prepare MTXNLCs, which was optimized using 3 2 full factorial designs. The mean diameter and surface morphology of MTXNLCs was evaluated. The crystallinity of lyophilized MTXNLCs was characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). MTXNLCs were integrated in 1% w/w Carbopol 934 P gel base, and in vitro skin deposition studies in human cadaver skin (HCS) were carried out. Results: The optimized MTXNLCs were rod-shaped, with an average particle size of 253 ± 8.65 nm, a zeta potential of −26.4±0.86 mV, and EE of 54.00±1.49%. DSC and XRD data confirmed the formation of NLCs. Significantly higher deposition of MTX was found in HCS from MTXNLC gel (71.52 ±1.13%) as compared to MTX plain gel (38.48±0.96%). In vivo studies demonstrated significant improvement in therapeutic response and reduction in local side effects with MTXNLCs-loaded gel in the topical treatment of psoriasis. Anti-psoriatic efficacy of MTXNLCs 100 ug/cm 2 compared with plain MTX gel was evaluated using imiquimod (IMQ)-induced psoriasis in BALB/c mice. The topical application of MTXNLCs to the mouse ear resulted in a significant reduction of psoriatic area and severity index, oxidative stress, inflammatory cytokines like TNF-α, IL-1β, and IL-6 and IMQ-induced histopathological alterations in mouse ear samples. Conclusion: Developed formulation of MTXNLC gel demonstrated better anti-psoriatic activity and also displayed prolonged and sustained release effect, which shows that it can be a promising alternative to existing MTX formulation for the treatment of psoriasis.

show abstract

“…SLN and NLC were prepared by high-speed homogenization and ultrasonication method [11]. Briefly, LX and phospholipon 90G were dissolved in methanol.…”

Section: Preparation Of Lx-loaded Sln and Nlcmentioning

confidence: 99%

“…The release medium was contained 25 ml of phosphate buffer (pH 7.4). At predetermined intervals 2 ml of samples were withdrawn from receptor compartment and replaced with equal volume of release medium [11].…”

Section: Preparation Of Lx-loaded Sln and Nlcmentioning

confidence: 99%

Rp-HPLC Method Development, Validation, and Quantification of Lornoxicam in Lipid Nanoparticle Formulations

Dasgupta

Dey²,

Pal

et al. 2016

Int J Pharm Pharm Sci

View full text Add to dashboard Cite

Objective: A simple, reliable, sensitive and validated reversed phase-high performance liquid chromatography (RP-HPLC) method was developed for quantification of lornoxicam (LX) in rat plasma.Methods: Solid lipid nanoparticle (SLN) and nanostructured lipid carriers (NLC) gel formulations containing lornoxicam were prepared using high-speed homogenization followed by ultra-sonication. Pharmacokinetic study of formulated LX loaded SLN and NLC were performed on Wister albino rats.Results: The chromatographic separation was performed on hypersil octadecylsilane (ODS)-18 column using a mobile phase of 10 mmol. Phosphate buffer (pH, 4.5) and acetonitrile (65:35 v/v). Elute was monitored at 377 nm with a flow rate of 1 ml/min. Calibration curve was linear over the concentration range of 25.38–2046.45 ng/ml. Retention times of LX and internal standard (piroxicam) were 9.3 and 10.2 min, respectively. Maximum plasma drug concentration, the area under the plasma drug concentration versus time curve and elimination half-life for LX loaded SLN gel were found 6381.51±971.27ng/ml, 19917.21±7111.24 ng h/ml and 7.27±1.21h and 8558.13±1564.08 ng/ml, 21317.99±4568.71 ng/ml and 6.22±2.16 h. respectively. In vivo in vitro correlation study, the fraction of drug dissolved from nanoparticle in pH 7.4 was plotted against the fraction of drug absorbed and a linear correlation (R2= 0.9987) was obtained.Conclusion: A novel simple, simple, sensitive, precise, rapid, accurate, and economical and reliable RP-HPLC method was developed and validated for the estimation of LX in rat plasma.

show abstract

Nanostructured lipid carriers (NLC) based topical gel of flurbiprofen: Design, characterization and in vivo evaluation

Cited by 95 publications

References 35 publications

Podophyllotoxin-Loaded Nanostructured Lipid Carriers for Skin Targeting: In Vitro and In Vivo Studies

Podophyllotoxin-Loaded Nanostructured Lipid Carriers for Skin Targeting: In Vitro and In Vivo Studies

<p>Methotrexate-Loaded Nanostructured Lipid Carrier Gel Alleviates Imiquimod-Induced Psoriasis by Moderating Inflammation: Formulation, Optimization, Characterization, In-Vitro and In-Vivo Studies</p>

Rp-HPLC Method Development, Validation, and Quantification of Lornoxicam in Lipid Nanoparticle Formulations

Contact Info

Product

Resources

About