Abstract:Objective:
Intraocular pressure has always been a great challenge for topical ophthalmic drugs. The study aimed to develop ocular surfactant based nanovesicles (NVs) carried in mucoadhesive nanogel providing efficient topical delivery of acetazolamide (ACZ).
Methods:
For the sake of optimizing formulation parameters, the effect of the type of edge activator and its ratio to sorbitan monostearate (Span 60) on the mean particle size, entrapment efficiency (%EE), and zeta potent… Show more
“…7,8 Recently, novel studies have been carried out to enhance the bioavailability, such as solid dispersion, 9 liposomes, 10 chitosan microparticles, 11 polymeric lipid-core nanocapsules, 12 and lipid vesicles. 13,15 Lipid vesicles, as a tool for drug delivery of SUT, have been studied. 16 Transferosomes are ultra-flexible and very deformable vesicles.…”
Background: Sumatriptan succinate (SUT) is a potent drug used for relieving or ending migraine and cluster headaches. SUT bioavailability is low (15%) when it is taken orally owing to its gastric breakdown and bloodstream before reaching the target arteries. Aim: The aim of the study was to enhance SUT bioavailability through developing an intranasal transferosomal mucoadhesive gel. Methods: SUT-loaded nanotransferosomes were prepared by thin film hydration method and characterized for various parameters such as vesicle diameter, percent entrapment efficiency (%EE), in vitro release and ex vivo permeation studies. The in-situ gels were prepared using various ratios of poloxamer 407, poloxamer 188, and carrageenan and characterized for gelation temperature, mucoadhesive strength, and rheological properties. Results: The prepared transferosomes exhibited percent entrapment efficiencies (%EE) of 40.41±3.02 to 77.47±2.85%, mean diameters of 97.25 to 245.01 nm, sustained drug release over 6 hours, and acceptable ex vivo permeation findings. The optimum formulae were incorporated into poloxamer 407 and poloxamer 188-based thermosensitive in-situ gel using carrageenan as a mucoadhesive polymer. Pharmacokinetic evaluation showed that the prepared in-situ gel of SUT-loaded nano-transferosomes gave enhanced bioavailability, 4.09fold, as compared to oral drug solution. Conclusion: Based on enhancing the bioavailability and sustaining the drug release, it can be concluded that the in-situ gel of SUT-loaded nano-transferosomes were developed as a promising non-invasive drug delivery system for treating migraine.
“…7,8 Recently, novel studies have been carried out to enhance the bioavailability, such as solid dispersion, 9 liposomes, 10 chitosan microparticles, 11 polymeric lipid-core nanocapsules, 12 and lipid vesicles. 13,15 Lipid vesicles, as a tool for drug delivery of SUT, have been studied. 16 Transferosomes are ultra-flexible and very deformable vesicles.…”
Background: Sumatriptan succinate (SUT) is a potent drug used for relieving or ending migraine and cluster headaches. SUT bioavailability is low (15%) when it is taken orally owing to its gastric breakdown and bloodstream before reaching the target arteries. Aim: The aim of the study was to enhance SUT bioavailability through developing an intranasal transferosomal mucoadhesive gel. Methods: SUT-loaded nanotransferosomes were prepared by thin film hydration method and characterized for various parameters such as vesicle diameter, percent entrapment efficiency (%EE), in vitro release and ex vivo permeation studies. The in-situ gels were prepared using various ratios of poloxamer 407, poloxamer 188, and carrageenan and characterized for gelation temperature, mucoadhesive strength, and rheological properties. Results: The prepared transferosomes exhibited percent entrapment efficiencies (%EE) of 40.41±3.02 to 77.47±2.85%, mean diameters of 97.25 to 245.01 nm, sustained drug release over 6 hours, and acceptable ex vivo permeation findings. The optimum formulae were incorporated into poloxamer 407 and poloxamer 188-based thermosensitive in-situ gel using carrageenan as a mucoadhesive polymer. Pharmacokinetic evaluation showed that the prepared in-situ gel of SUT-loaded nano-transferosomes gave enhanced bioavailability, 4.09fold, as compared to oral drug solution. Conclusion: Based on enhancing the bioavailability and sustaining the drug release, it can be concluded that the in-situ gel of SUT-loaded nano-transferosomes were developed as a promising non-invasive drug delivery system for treating migraine.
“…These findings could be related to the mucoadhesive and viscosity-inducing properties of HPMC which can markedly prolong the drug residence time in the conjunctival sac and allow more time for the drug to diffuse via the ocular layers. The advantages of the incorporation of nanostructured systems in HPMC ocular systems were previously reported for many drugs like levofloxacin hemihydrate, 67 acetazolamide, 68 and voriconazole. 69 …”
Aim
Norfloxacin (NFX) has low ocular bioavailability. The current work aimed to develop NFX-loaded nanoparticle (NP)-laden hydrogels to improve the ocular potential of NFX, minimize the need for frequent instillations and lower undesirable side effects.
Methods
NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 2
1
.4
1
full factorial design, using two types of polylactic-co-glycolic acid (PLGA) polymer and four (drug: polymer) ratios. NPs were evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), drug entrapment efficiency percentage (EE%), drug percentage released after 30 min (Q
30min
) and 12 hours (Q
12h
), drug percentage permeated through goat corneas after 30 min (P
30min
) and 12 hours (P
12h
) and morphology. Two formulae were statistically selected and incorporated into hydroxypropyl methylcellulose (HPMC)-based hydrogels; G1 – G4. The latter systems were evaluated for appearance, clarity, pH, spreadability, rheology, drug percentages released, drug percentages permeated, antimicrobial activity against
Pseudomonas aeruginosa
, and histopathological changes.
Results
The selected NPs (NP2 and NP6) were spherical in shape and possessed suitable PS (392.02 nm and 190.51 nm) and PDI (0.17 and 0.18), high magnitude of ZP (−30.43 mV and −33.62 mV), high EE% (79.24% and 91.72%), low Q
30min
(10.96% and 16.65%) and P
30min
(17.39% and 21.05%) and promising Q
12h
(58.23% and 71.20%) and P
12h
(53.31% and 65.01%), respectively. Clear, spreadable, tolerable, pseudoplastic, and thixotropic HPMC-based hydrogels were developed. They showed more prolonged drug release and drug permeation profiles. NP2- and NP6-laden hydrogels (G3 and G4 systems, respectively) had promising antibacterial activity, and reasonable histopathological safety.
Conclusion
G3 and G4 are potential ocular delivery systems for NFX.
“… 50 Proinflammatory cytokines, including IL6, IL10, IL1β, and TNFα, stimulate muscle-protein degradation, cause contractile dysfunction, and inhibit myogenesis, in addition to promoting adipose-tissue waste, inhibition of adipocyte differentiation, lipolysis stimulation, and increased apoptosis in adipocytes. 51 Figure 12 Weight loss recorded for groups treated with control (isotonic saline solution), free GMC, GMC LPs, GMC-Fo LPs, and GMC-SoS-Fo LPs without ultrasonic irradiation and GMC-SoS-Fo LPs with ultrasonic irradiation) in xenograft ovarian cancer rat models. Results depicted as the means ± SD (n=10).…”
Purpose
To develop an externally triggered rapid-release targeted system for treating ovarian cancer, gemcitabine (GMC) was entrapped into sonosensitive (SoS) folate (Fo)-modified liposomes (LPs).
Methods
GMC-loaded LPs (GMC LPs), GMC-loaded Fo-targeted LPs (GMC-Fo LPs), and GMC-loaded Fo-targeted SoS LPs (GMC-SoS Fo LPs) were prepared utilizing a film-hydration technique and evaluated based on particle size, ζ-potential, and percentage entrapped drug. Cellular uptake of the fluorescent delivery systems in Fo-expressing ovarian cancer cells was quantified using flow cytometry. Finally, tumor-targeting ability, in vivo evaluation, and pharmacokinetic studies were performed.
Results
GMC LPs, GMC-Fo LPs, and GMC-SoS Fo LPs were successfully prepared, with sizes of <120.3±2.4 nm, 39.7 mV ζ-potential, and 86.3%±1.84% entrapped drug. Cellular uptake of GMC-SoS Fo LPs improved 6.51-fold over GMC LPs (under ultrasonic irradiation —
p
<0.05). However, cellular uptake of GMC-Fo LPs improved just 1.24-fold over GMC LPs (
p
>0.05). Biodistribution study showed that of GMC concentration in tumors treated with GMC-SoS-Fo LPs (with ultrasound) improved 2.89-fold that of free GMC (
p
<0.05). In vivo, GMC-SoS Fo LPs showed the highest antiproliferative and antitumor action on ovarian cancer.
Conclusion
These findings showed that externally triggered rapid-release SoS Fo-modified LPs are a promising system for delivering rapid-release drugs into tumors.
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