Bioadhesive microspheres as a potential nasal drug delivery system

Illum, Lisbeth; Jørgensen, H.; Bisgaard, Hans; Krogsgaard, O.; Rossing, Niels Nygaard

doi:10.1016/0378-5173(87)90216-x

Cited by 214 publications

(60 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Smaller-sized particles are benefited by EPR effect as they tend to accumulate in the tumor sites. Particles 51 lm are capable of passing through the nasal cavities with the inspired air, whereas particles 410 lm gets deposited at the anterior parts of the nose and thus evades ciliated absorption areas (Illum et al, 1987). The zeta potential for optimized formulation CPC-08 was À16.3 ± 3.7 mV, which was due to the negative charge of PCL.…”

Section: Entrapment Efficiencymentioning

confidence: 90%

Development and evaluation of carboplatin-loaded PCL nanoparticles for intranasal delivery

Alex

Joseph

Shavi³

et al. 2014

Drug Delivery

109

View full text Add to dashboard Cite

Context: The study was aimed to develop a polymeric nanoparticle formulation of anticancer drug carboplatin using biodegradable polymer polycaprolactone (PCL). The formulation is intended for intranasal administration to treat glioma anticipating improved brain delivery as nasal route possess direct access to brain and nanoparticles have small size to overcome the mucosal and blood-brain barrier. Objective: Development and evaluation of carboplatin-PCL nanoparticles for brain delivery by nasal route. Methodology: Carboplatin-loaded PCL nanoparticles (CPCs) were prepared by double emulsionsolvent evaporation technique and characterized by particle size, zeta potential, entrapment efficiency, scanning electron microscopy and differential scanning calorimetry. The CPCs were assessed for in vitro release kinetics, ex vivo permeation and in situ nasal perfusion. Cytotoxic potential of CPCs in vitro was evaluated on LN229 human glioblastoma cells. Results and discussion: The optimized formulation of carboplatin-PCL nanoparticle CPC-08 with particle size of 311.6 ± 4.7 nm and zeta potential À16.3 ± 3.7 mV exhibited percentage entrapment efficiency of 27.95 ± 4.21. In vitro drug release showed initial burst release followed by slow and continues release indicating biphasic pattern. The ex vivo permeation pattern through sheep nasal mucosa also exhibited a similar release pattern as for in vitro release studies. In situ nasal perfusion studies in Wistar rats demonstrate that CPCs show better nasal absorption than carboplatin solution. In vitro cytotoxicity studies on LN229 cells showed an enhancement in cytotoxicity by CPCs compared to carboplatin alone. Conclusion: CPC-08 effectively improves nasal absorption of carboplatin and can be used for intranasal administration of carboplatin for improved brain delivery.

show abstract

Section: Entrapment Efficiencymentioning

confidence: 90%

Development and evaluation of carboplatin-loaded PCL nanoparticles for intranasal delivery

Alex

Joseph

Shavi³

et al. 2014

Drug Delivery

109

View full text Add to dashboard Cite

show abstract

“…The mean particle size of microsperes ranged from 9, 5 to 11.5μm (Table 2). It has been suggested that 10μm particle size is most suitable for nasal administration [15]. …”

Section: Particle Size Measurementmentioning

confidence: 99%

Formulation of sildenafil citrate loaded nasal microsphers: An in vitro, ex vivo characterization.

Shah¹,

Sharma²,

Vijay³

et al. 2010

Int j Drug delivery

View full text Add to dashboard Cite

The aim of the present study was to prepare gellan gum microspheres of Sildenafil citrate, for intranasal delivery to avoid the first pass metabolism. The microspheres were prepared using spray drying method. The microspheres were evaluated for characteristics like particle size, incorporation efficiency, swelling ability, zeta potential, in-vitro mucoadhesion, ex-vivo mucoadhesion, thermal analysis, XRD study and invitro drug release. Treatment of in-vitro data to different kinetic equations indicated diffusion controlled drug delivery from gellan gum microspheres. The results of DSC and XRD studies revealed the molecular amorphous dispersion of Sildenafil citrate into the gellan gum microspheres. Microspheres so prepared were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 95-98%. The formulation exhibited a good mucoadhesive strength which was determined in in vitro conditions through falling film technique and was compared with ex vivo studies. The microspheres so prepared also exhibited a good swelling index which confirmed the strong mucoadhesive property of the formulation.

show abstract

“…19) Microspheres prepared with mucoadhesive and bioerodable polymers undergo selective uptake by the M cells of Peyer patches in gastrointestinal (GI) mucosa. 20) This uptake mechanism has been used for the delivery of protein and peptide drugs, antigens for vaccination and plasmid DNA for gene therapy.…”

Section: ) Mucoadhesive Microspheresmentioning

confidence: 99%

Mucoadhesive Microspheres for Controlled Drug Delivery

Chowdary

Rao

2004

Biological & Pharmaceutical Bulletin

153

View full text Add to dashboard Cite

Mucoadhesion is a topic of current interest in the design of drug delivery systems. Mucoadhesive microspheres exhibit a prolonged residence time at the site of application or absorption and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved and/or better therapeutic performance of drugs. In recent years such mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal routes for either systemic or local effects. The objective of this article is review the principles underlying the development and evaluation of mucoadhesive microspheres and the research work carried out on these systems.

show abstract

Bioadhesive microspheres as a potential nasal drug delivery system

Cited by 214 publications

References 18 publications

Development and evaluation of carboplatin-loaded PCL nanoparticles for intranasal delivery

Development and evaluation of carboplatin-loaded PCL nanoparticles for intranasal delivery

Formulation of sildenafil citrate loaded nasal microsphers: An in vitro, ex vivo characterization.

Mucoadhesive Microspheres for Controlled Drug Delivery

Contact Info

Product

Resources

About