Development, Characterization, and Evaluation of SLN-Loaded Thermoresponsive Hydrogel System of Topotecan as Biological Macromolecule for Colorectal Delivery

Xing, Ronge; Mustapha, Omer; Ali, Tariq; Rehman, Maqsood Ur; Zaidi, Syed Saoud; Baseer, Abdul; Batool, Sibgha; Mukhtiar, Muhammad; Shafique, Shumaila; Malik, Maria Saleem; Sohail, Saba; Ali, Zameer; Zahid, Fatima; Zeb, Alam; Shah, Fawad Ali; Abid, Sharjeel; Din, Fakhar ud

doi:10.1155/2021/9968602

Cited by 39 publications

(22 citation statements)

References 57 publications

(75 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In contrast, the diffraction pattern of IBU-SLNs is amorphous and only characterized by large diffraction peaks, while the characteristic peaks of IBU and lipids do not exist. 40 The disappearance of IBU peak observed in the IBU-SLNs indicated that there was no IBU peak in the crystalline state in the SLNs. 41 This may be attributed to the incorporation of IBU into the lipid matrix and successful encapsulation of the drug inside the lipids.…”

Section: Resultsmentioning

confidence: 95%

Preparation, in vitro and in vivo Evaluation of Thermosensitive in situ Gel Loaded with Ibuprofen-Solid Lipid Nanoparticles for Rectal Delivery

Huang¹,

Hu²,

Wu³

et al. 2022

DDDT

View full text Add to dashboard Cite

Background Ibuprofen (IBU), a nonsteroidal anti-inflammatory drug, shows poor gastrointestinal absorption due to its low solubility, which limits its clinical application. Objective In the present study, we aimed to develop thermosensitive gel-mediated ibuprofen-solid lipid nanoparticles (IBU-SLN-ISG) to improve the dissolution and bioavailability of IBU after rectal delivery. Methods IBU-loaded SLNs (IBU-SLNs) were developed and optimized applying Box-Behnken design. The optimized IBU-SLNs were characterized by physicochemical parameters and morphology. Then, the optimized IBU-SLNs was incorporated into the gel and characterized for gel properties and rheology and investigated its release in vitro, pharmacokinetics in vivo, rectal irritation and rectal retention time. Results The optimized SLNs had an EE of 90.74 ± 1.40%, DL of 11.36 ± 1.20%, MPS of 166.77 ± 2.26 nm, PDI of 0.27 ± 0.08, and ZP of −21.00 ± 0.59 mV. The FTIR spectra confirmed successful encapsulation of the drug inside the nanoparticle as only peaks responsible for the lipid could be identified. This corroborated well with XRD spectra, which showed a completely amorphous state of the IBU-SLNs as compared to the crystalline nature of the pure drug. The gelation temperature of the prepared IBU-SLN-ISG was 33.30 ± 0.78°C, the gelation time was 14.67 ± 2.52 s, the gel strength was 54.00 ± 1.41 s, and the mucoadhesion was (11.54±0.37) × 10 2 dyne/cm 2 . The in vitro results of IBU-SLNs and IBU-SLN-ISG showed a biphasic release pattern with initial burst release followed by sustained release. More importantly, IBU-SLN-ISG produced much better absorption of IBU and improved bioavailability in rats. In addition, IBU-SLN-ISG caused no irritation or damage to rectal tissues, and could be retained in the rectum for a long time. Conclusion Thermosensitive in situ gel loaded with IBU-solid lipid nanoparticles might be further developed as a more convenient and effective rectal dosage form.

show abstract

Section: Resultsmentioning

confidence: 95%

Preparation, in vitro and in vivo Evaluation of Thermosensitive in situ Gel Loaded with Ibuprofen-Solid Lipid Nanoparticles for Rectal Delivery

Huang¹,

Hu²,

Wu³

et al. 2022

DDDT

View full text Add to dashboard Cite

show abstract

“…The images showed increase in the particle size with the increasing concentration of chitosan while no intraparticle interaction was observed. TEM images demonstrated the nanosize and uniform distribution of the SLNs while the influence of chitosan coating in an increase in the particle size was also observed which was due to the formation of chitosan layers over the particles [ 48 , 49 ].…”

Section: Resultsmentioning

confidence: 99%

Physicochemical Characterization of Chitosan-Decorated Finasteride Solid Lipid Nanoparticles for Skin Drug Delivery

Sohaib

Shah

et al. 2022

BioMed Research International

View full text Add to dashboard Cite

Finasteride is considered the drug of choice for androgenic alopecia and benign prostate hyperplasia. The aim of the study was to formulate nanodrug carriers of finasteride with enhanced retentive properties in the skin. The finasteride was formulated as solid lipid nanoparticles that were decorated with different concentrations of chitosan for improved retentive properties. Solid lipid nanoparticles (SLNs) were synthesized by “high-speed homogenization technique” using stearic acid as a solid lipid while PEG-6000 and Tween-80 were used as surfactants. The SLNs were evaluated for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, and drug release behavior. The mean particle size of SLNs was in the range of 10.10 nm to 144.2 nm. The PDI ranged from 0.244 to 0.412 while zeta potential was in the range of 8.9 mV to 62.6 mV. The drug entrapment efficiency in chitosan undecorated formulations was 48.3% while an increase in drug entrapment was observed in chitosan-decorated formulations (51.1% to 62%). The in vitro drug release studies of SLNs showed an extended drug release for 24 hours after 4 hours of initial burst release. The extended drug release was observed in chitosan-coated SLNs in comparison with uncoated nanoparticles. The permeation and retention study revealed higher retention of drug in the skin and low permeation with chitosan-decorated SLNs that ranged from 39.4 μg/cm2 to 13.2 μg/cm2. TEM images depicted spherical shape of SLNs. The stability study confirmed stable formulations in temperature range of 5°C and 40°C for three months. It is concluded from this study that the SLNs of finasteride were successfully formulated and chitosan decoration enhanced the drug retention in the skin layers. Therefore, these formulations could be used in androgenic alopecia and benign prostate hyperplasia to avoid the side effects, drug degradation, and prolonged use of drug with conventional oral therapy.

show abstract

“…ZP is measured to assess the surface charge of the particle and the value ±30 mV is ideal for the stability of NPs. The sample is diluted and transferred to a cuvette (contain electrode) and placed into an instrument to analyze the result in triplicate (Xing et al., 2021 ).…”

Section: Methodsmentioning

confidence: 99%

Formulation and evaluation of butenafine loaded PLGA-nanoparticulate laden chitosan nano gel

Alshehri

Imam

2021

Drug Delivery

View full text Add to dashboard Cite

Development, Characterization, and Evaluation of SLN-Loaded Thermoresponsive Hydrogel System of Topotecan as Biological Macromolecule for Colorectal Delivery

Cited by 39 publications

References 57 publications

Preparation, in vitro and in vivo Evaluation of Thermosensitive in situ Gel Loaded with Ibuprofen-Solid Lipid Nanoparticles for Rectal Delivery

Preparation, in vitro and in vivo Evaluation of Thermosensitive in situ Gel Loaded with Ibuprofen-Solid Lipid Nanoparticles for Rectal Delivery

Physicochemical Characterization of Chitosan-Decorated Finasteride Solid Lipid Nanoparticles for Skin Drug Delivery

Formulation and evaluation of butenafine loaded PLGA-nanoparticulate laden chitosan nano gel

Contact Info

Product

Resources

About