Noha Nafee | Kuwait University (original) (raw)
Papers by Noha Nafee
SUMMARY The hydrophobic nature of aluminium phthalocyanine causes its aggregation in biological f... more SUMMARY The hydrophobic nature of aluminium phthalocyanine causes its aggregation in biological fluids, thus abolishes its photoactivity and limits its biological application. Amphiphilic biodegradable block copolymers were synthesized and allowed to assemble in aqueous solution into nanoparticles (<100 nm). AlPc encapsulated in these polymeric nanoparticles exhibit better photodynamic activity, lower dark toxicity and prolonged release behavior compared to the free photosensitizer. Amphiphilic nanoparticles could be considered a promising carrier for hydrophobic photosensitizers.
SUMMARY Plain solid lipid nanoparticles (SLNs) were formulated by melt emulsification method usin... more SUMMARY Plain solid lipid nanoparticles (SLNs) were formulated by melt emulsification method using different lipids, fatty acids and waxes stabilized by polymeric emulsifying agents. The optimized nanoparticles were spherical in the size range of 100-200 nm with narrow size distribution as confirmed by polydispersity index (PDI < 0.2). SLNs were negatively charged with ζ-potential values between -3 and -18 mV. Amphiphilic lipids provided smaller and more stable SLNs compared to fatty acids and waxes. For the pulmonary delivery purposes, SLNs were nebulized using jet nebulizers. Results showed promising aerosol output rate as well as colloidal stability. INTRODUCTION Currently, lipid-based nanocarriers including SLNs and Nano-structured lipid carriers (NLCs) become an appealing advance in versatile pharmaceutical applications [1]. SLNs consist of nanosized solid lipid particles dispersed in aqueous medium. SLNs have the advantages of acquisition of biocompatible and biodegradable ...
European Journal of Pharmaceutics and Biopharmaceutics, 2018
Colloids and surfaces. B, Biointerfaces, Jan 10, 2015
A series of cyclodextrin-based star polymers were synthesized using β-cyclodextrin (CD) as hydrop... more A series of cyclodextrin-based star polymers were synthesized using β-cyclodextrin (CD) as hydrophilic core, methyl methacrylate (MMA) and tert-butyl acrylate (tBA) as hydrophobic arms. Star polymers, either homopolymers or random/block copolymers, showed narrow molecular weight distributions. Grafting hydrophobic arms created CD-based nanoparticles (CD-NPs) in the size range (130-200nm) with narrow PdI <0.15 and slightly negative ζ-potential. Particle surface could be modified with chitosan to impart a positive surface charge. Colloidal stability of CD-NPs was a function of pH as revealed by the pH-titration curves. CD-NPs were used as carrier for the chemotherapeutic drug idarubicin (encapsulation efficiency, EE ∼40%) ensuring prolonged release profile (∼80% after 48h). For cell-based studies, coumarin-6 was encapsulated as a fluorescent marker (EE ∼75%). Uptake studies carried out on A549 and Caco-2 cell lines proved the uptake of coumarin-loaded NPs as a function of time and ...
European Journal of Pharmaceutics and Biopharmaceutics, 2012
International Journal of Pharmaceutics, 2011
Journal of Controlled Release
AAPS PharmSciTech, 2020
Non-invasive brain therapy for chronic neurological disorders is in high demand. Vinpocetine (VIN... more Non-invasive brain therapy for chronic neurological disorders is in high demand. Vinpocetine (VIN) tablets for cerebrovascular degenerative disorders ensued < 7% oral bioavailability. The olfactory pathway (providing direct brain access) can improve VIN pharmacokinetic/pharmacodynamic profile. In this context, VIN hydrogels based on temperature-, pH-, and ion-triggered gelation in physiological milieu were formulated. Poloxamer-chitosan (PLX-CS) and carbopol-HPMC-alginate (CP-HPMC-SA) systems were optimized for appropriate gelation time, temperature, and pH. PLX-CS-hydrogels exhibited strong mucoadhesion for > 8 h, while CP-HPMC-SA hydrogels were mucoadhesive in simulated nasal fluid, owing to pH and ion-activated gelation. Along with prolonged mucosal residence, hydrogels confirmed sustained VIN release (> 24 h), especially from CP-HPMC-SA hydrogels. As proof of concept, brain exposure of intranasal VIN hydrogels was investigated in rats versus VIN-IV bolus. PLX-CS provided 146% increase in AUC0-30 and 3-fold maximum brain concentration (BCmax) relative to IV bolus. BCmax was reached after 4 h versus 1 h (IV bolus). CP-HPMC-SA hydrogel showed superior brain targeting efficiency (460%) and brain direct transport percentage (78.23%). VIN plasma pharmacokinetics confirmed 45-60% reduction in AUCplasma versus IV bolus, while PCmax of CP-HPMC-SA and PLX-CS represented 17 and 28% that of IV bolus, respectively. Olfactory-targeted hydrogels grant effective, sustainable VIN brain level with minimal systemic exposure, thus, assuring lower dose, dose frequency, side effects, and per se better patient compliance.
British Journal of Pharmacy, 2019
European Journal of Pharmaceutical Sciences, 2017
Journal of Liposome Research, 2017
Photodiagnosis and Photodynamic Therapy, 2016
International Journal of Pharmaceutics, 2015
International journal of pharmaceutics, Jan 10, 2015
Whether mini-tablets (tablets, diameters ≤6mm) belong to single- or multiple-unit dosage forms is... more Whether mini-tablets (tablets, diameters ≤6mm) belong to single- or multiple-unit dosage forms is still questionable. Accordingly, Pharmacopoeial evaluation procedures for mini-tablets are lacking. In this study, the aforementioned points were discussed. Moreover, their potential for oral controlled delivery was assessed. The antidepressant venlafaxine hydrochloride (Vx), a highly soluble drug undergoing first pass effect, low bioavailability and short half-life was selected as a challenging payload. In an attempt to weigh up mini-tablets versus pellets as multiparticulate carriers, Vx-loaded mini-tablets were compared to formulated pellets of the same composition and the innovator Effexor(®)XR pellets. Formulations were prepared using various polymer hydrogels in the core and ethyl cellulose film coating with increasing thickness. Mini-tablets (diameter 2mm) showed extended Vx release (<60%, 8h). Indeed, release profiles comparable to Effexor(®)XR pellets were obtained. Remarkab...
International Journal of Pharmaceutics, 2013
ABSTRACT
ABSTRACT Respiratory mucus is one of the main barriers for nanoparticle-based pulmonary delivery ... more ABSTRACT Respiratory mucus is one of the main barriers for nanoparticle-based pulmonary delivery systems. This holds true especially for lung diseases like cystic fibrosis, where a very tenacious thick mucus layer hinders particle diffusion to the lung epithelium or the target area. Typically, mean square displacement of particles is used for mobility evaluation. In contrast, our objective is to develop a feasible technique to track directed particle penetration as a prerequisite for efficient pulmonary nanotherapy. Therefore, particle diffusion in artificial mucus was monitored based on confocal laser scanning microscopy (CLSM) and particle-mucus interaction was observed. As pharmaceutical relevant and benign materials, solid lipid nanoparticles (SLNs) were prepared by hot-melt emulsification using glyceryl behenate and different stabilizing agents such as poloxamer-407, tween-80, and polyvinyl alcohol (PVA). The diffusion of labeled SLNs in stained artificial sputum representing CF-patient sputum was verified by 3D time laps imaging. Thus, the effect of coating, particle size and mucus viscosity on nanoparticle diffusion was studied. Using image analysis software "Image J", the total fluorescent signal after 30 min in case of poloxamer-coated SLNs was 5 and 100 folds higher than tween- and PVA-coated SLNs, respectively. Nevertheless, increasing mucus viscosity reduced the diffusion of tweencoated SLNs by a factor of 10. Studying particle-mucus interaction by CLSM can be considered a promising and versatile technique.
Nanotherapeutics - Drug Delivery Concepts in Nanoscience
... The contact time of the carrier systems with the membrane might increase uptake probability P... more ... The contact time of the carrier systems with the membrane might increase uptake probability Page 58. Transport Across Biological Barriers 45 [El-Shabouri, 2002; Hariharan et al, 2006]. ... 787-792. Bharali, DJ, Lucey, DW, Jayakumar, H., Pudavar, HE and Prasad, PN (2005). ...
SUMMARY The hydrophobic nature of aluminium phthalocyanine causes its aggregation in biological f... more SUMMARY The hydrophobic nature of aluminium phthalocyanine causes its aggregation in biological fluids, thus abolishes its photoactivity and limits its biological application. Amphiphilic biodegradable block copolymers were synthesized and allowed to assemble in aqueous solution into nanoparticles (<100 nm). AlPc encapsulated in these polymeric nanoparticles exhibit better photodynamic activity, lower dark toxicity and prolonged release behavior compared to the free photosensitizer. Amphiphilic nanoparticles could be considered a promising carrier for hydrophobic photosensitizers.
SUMMARY Plain solid lipid nanoparticles (SLNs) were formulated by melt emulsification method usin... more SUMMARY Plain solid lipid nanoparticles (SLNs) were formulated by melt emulsification method using different lipids, fatty acids and waxes stabilized by polymeric emulsifying agents. The optimized nanoparticles were spherical in the size range of 100-200 nm with narrow size distribution as confirmed by polydispersity index (PDI < 0.2). SLNs were negatively charged with ζ-potential values between -3 and -18 mV. Amphiphilic lipids provided smaller and more stable SLNs compared to fatty acids and waxes. For the pulmonary delivery purposes, SLNs were nebulized using jet nebulizers. Results showed promising aerosol output rate as well as colloidal stability. INTRODUCTION Currently, lipid-based nanocarriers including SLNs and Nano-structured lipid carriers (NLCs) become an appealing advance in versatile pharmaceutical applications [1]. SLNs consist of nanosized solid lipid particles dispersed in aqueous medium. SLNs have the advantages of acquisition of biocompatible and biodegradable ...
European Journal of Pharmaceutics and Biopharmaceutics, 2018
Colloids and surfaces. B, Biointerfaces, Jan 10, 2015
A series of cyclodextrin-based star polymers were synthesized using β-cyclodextrin (CD) as hydrop... more A series of cyclodextrin-based star polymers were synthesized using β-cyclodextrin (CD) as hydrophilic core, methyl methacrylate (MMA) and tert-butyl acrylate (tBA) as hydrophobic arms. Star polymers, either homopolymers or random/block copolymers, showed narrow molecular weight distributions. Grafting hydrophobic arms created CD-based nanoparticles (CD-NPs) in the size range (130-200nm) with narrow PdI <0.15 and slightly negative ζ-potential. Particle surface could be modified with chitosan to impart a positive surface charge. Colloidal stability of CD-NPs was a function of pH as revealed by the pH-titration curves. CD-NPs were used as carrier for the chemotherapeutic drug idarubicin (encapsulation efficiency, EE ∼40%) ensuring prolonged release profile (∼80% after 48h). For cell-based studies, coumarin-6 was encapsulated as a fluorescent marker (EE ∼75%). Uptake studies carried out on A549 and Caco-2 cell lines proved the uptake of coumarin-loaded NPs as a function of time and ...
European Journal of Pharmaceutics and Biopharmaceutics, 2012
International Journal of Pharmaceutics, 2011
Journal of Controlled Release
AAPS PharmSciTech, 2020
Non-invasive brain therapy for chronic neurological disorders is in high demand. Vinpocetine (VIN... more Non-invasive brain therapy for chronic neurological disorders is in high demand. Vinpocetine (VIN) tablets for cerebrovascular degenerative disorders ensued < 7% oral bioavailability. The olfactory pathway (providing direct brain access) can improve VIN pharmacokinetic/pharmacodynamic profile. In this context, VIN hydrogels based on temperature-, pH-, and ion-triggered gelation in physiological milieu were formulated. Poloxamer-chitosan (PLX-CS) and carbopol-HPMC-alginate (CP-HPMC-SA) systems were optimized for appropriate gelation time, temperature, and pH. PLX-CS-hydrogels exhibited strong mucoadhesion for > 8 h, while CP-HPMC-SA hydrogels were mucoadhesive in simulated nasal fluid, owing to pH and ion-activated gelation. Along with prolonged mucosal residence, hydrogels confirmed sustained VIN release (> 24 h), especially from CP-HPMC-SA hydrogels. As proof of concept, brain exposure of intranasal VIN hydrogels was investigated in rats versus VIN-IV bolus. PLX-CS provided 146% increase in AUC0-30 and 3-fold maximum brain concentration (BCmax) relative to IV bolus. BCmax was reached after 4 h versus 1 h (IV bolus). CP-HPMC-SA hydrogel showed superior brain targeting efficiency (460%) and brain direct transport percentage (78.23%). VIN plasma pharmacokinetics confirmed 45-60% reduction in AUCplasma versus IV bolus, while PCmax of CP-HPMC-SA and PLX-CS represented 17 and 28% that of IV bolus, respectively. Olfactory-targeted hydrogels grant effective, sustainable VIN brain level with minimal systemic exposure, thus, assuring lower dose, dose frequency, side effects, and per se better patient compliance.
British Journal of Pharmacy, 2019
European Journal of Pharmaceutical Sciences, 2017
Journal of Liposome Research, 2017
Photodiagnosis and Photodynamic Therapy, 2016
International Journal of Pharmaceutics, 2015
International journal of pharmaceutics, Jan 10, 2015
Whether mini-tablets (tablets, diameters ≤6mm) belong to single- or multiple-unit dosage forms is... more Whether mini-tablets (tablets, diameters ≤6mm) belong to single- or multiple-unit dosage forms is still questionable. Accordingly, Pharmacopoeial evaluation procedures for mini-tablets are lacking. In this study, the aforementioned points were discussed. Moreover, their potential for oral controlled delivery was assessed. The antidepressant venlafaxine hydrochloride (Vx), a highly soluble drug undergoing first pass effect, low bioavailability and short half-life was selected as a challenging payload. In an attempt to weigh up mini-tablets versus pellets as multiparticulate carriers, Vx-loaded mini-tablets were compared to formulated pellets of the same composition and the innovator Effexor(®)XR pellets. Formulations were prepared using various polymer hydrogels in the core and ethyl cellulose film coating with increasing thickness. Mini-tablets (diameter 2mm) showed extended Vx release (<60%, 8h). Indeed, release profiles comparable to Effexor(®)XR pellets were obtained. Remarkab...
International Journal of Pharmaceutics, 2013
ABSTRACT
ABSTRACT Respiratory mucus is one of the main barriers for nanoparticle-based pulmonary delivery ... more ABSTRACT Respiratory mucus is one of the main barriers for nanoparticle-based pulmonary delivery systems. This holds true especially for lung diseases like cystic fibrosis, where a very tenacious thick mucus layer hinders particle diffusion to the lung epithelium or the target area. Typically, mean square displacement of particles is used for mobility evaluation. In contrast, our objective is to develop a feasible technique to track directed particle penetration as a prerequisite for efficient pulmonary nanotherapy. Therefore, particle diffusion in artificial mucus was monitored based on confocal laser scanning microscopy (CLSM) and particle-mucus interaction was observed. As pharmaceutical relevant and benign materials, solid lipid nanoparticles (SLNs) were prepared by hot-melt emulsification using glyceryl behenate and different stabilizing agents such as poloxamer-407, tween-80, and polyvinyl alcohol (PVA). The diffusion of labeled SLNs in stained artificial sputum representing CF-patient sputum was verified by 3D time laps imaging. Thus, the effect of coating, particle size and mucus viscosity on nanoparticle diffusion was studied. Using image analysis software "Image J", the total fluorescent signal after 30 min in case of poloxamer-coated SLNs was 5 and 100 folds higher than tween- and PVA-coated SLNs, respectively. Nevertheless, increasing mucus viscosity reduced the diffusion of tweencoated SLNs by a factor of 10. Studying particle-mucus interaction by CLSM can be considered a promising and versatile technique.
Nanotherapeutics - Drug Delivery Concepts in Nanoscience
... The contact time of the carrier systems with the membrane might increase uptake probability P... more ... The contact time of the carrier systems with the membrane might increase uptake probability Page 58. Transport Across Biological Barriers 45 [El-Shabouri, 2002; Hariharan et al, 2006]. ... 787-792. Bharali, DJ, Lucey, DW, Jayakumar, H., Pudavar, HE and Prasad, PN (2005). ...