Enhanced transdermal permeation of rasagiline mesylate nanoparticles: design, optimization, and effect of binary combinations of solvent systems across biological membrane

Bali, Nikhil; Shinde, Mahesh; Rathod, Shahadev B.; Salve, Pramod S.

doi:10.1080/00914037.2019.1706507

Cited by 10 publications

(1 citation statement)

References 48 publications

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“…These drug products leaves gastrointestinal tract (G.I.T) before the dissolution and originate inadequate ADME properties leading to reduced clinical effects and dosage escalation [5,6]. Various strategies have been investigated for solubility enhancement such as polymeric composites [7], polymeric nanoparticles [8], polymeric microneedles [9], polymeric microbeads [10], cocrystals [11], solid lipid nanoparticles (SLNs) [12], micelles [13], hydrogels [14], amorphous solid dispersions [12], liposome [15], nanosuspension [16], nanoemulsion, nanoplex [17],…”

Section: Introductionmentioning

confidence: 99%

Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug’s Solubility Improvement

Minhas

Khan

Sarfraz

et al. 2022

BioMed Research International

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Poor solubility is a global issue of copious pharmaceutical industries as large number of drugs in development stage as well as already marketed products are poorly soluble which results in low dissolution and ultimately dosage increase. Current study is aimed at developing a polyvinylpyrrolidone- (PVP-K30-) based nanogel delivery system for solubility enhancement of poorly soluble drug olanzapine (OLP), as solubilization enhancement is the most noteworthy application of nanosystems. Crosslinking polymerization with subsequent condensation technique was used for the synthesis of nanogels, a highly responsive polymeric networks in drug’s solubility. Developed nanogels were characterized by percent entrapment efficiency, sol-gel, percent swelling, percent drug loaded content (%DLC), percent porosity, stability, solubility, in vitro dissolution studies, FTIR, XRD, and SEM analysis. Furthermore, cytotoxicity study was conducted on rabbits to check the biocompatibility of the system. Particle size of nanogels was found with 178.99 ± 15.32 nm , and in vitro dissolution study exhibited that drug release properties were considerably enhanced as compared to the marketed formulation OLANZIA. The solubility studies indicated that solubility of OLP was noticeably improved up to 36.7-fold in phosphate buffer of pH 6.8. In vivo cytotoxicity study indicated that prepared PVP-K30-based formulation was biocompatible. On the basis of results obtained, the developed PVP-K30-co-poly (AMPS) nanogel delivery system is expected to be safe, effective, and cost-effective for solubility improvement of poorly soluble drugs.

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Section: Introductionmentioning

confidence: 99%

Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug’s Solubility Improvement

Minhas

Khan

Sarfraz

et al. 2022

BioMed Research International

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Thin film hydration versus modified spraying technique to fabricate intranasal spanlastic nanovesicles for rasagiline mesylate brain delivery: Characterization, statistical optimization, and in vivo pharmacokinetic evaluation

Ali

Shoukri

Yousry

2022

Drug Deliv. and Transl. Res.

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Rasagiline mesylate (RM) is a monoamine oxidase inhibitor that is commonly used to alleviate the symptoms of Parkinson’s disease. However, it suffers from low oral bioavailability due to its extensive hepatic metabolism in addition to its hydrophilic nature which limits its ability to pass through the blood–brain barrier (BBB) and reach the central nervous system where it exerts its pharmacological effect. Thus, this study aims to form RM-loaded spanlastic vesicles for intranasal (IN) administration to overcome its hepatic metabolism and permit its direct delivery to the brain. RM-loaded spanlastics were prepared using thin film hydration (TFH) and modified spraying technique (MST). A 23 factorial design was constructed to study and optimize the effects of the independent formulation variables, namely, Span type, Span: Brij 35 ratio, and sonication time on the vesicles᾽ characteristics in each preparation technique. The optimized system prepared using MST (MST 2) has shown higher desirability factor with smaller PS and higher EE%; thus, it was selected for further in vivo evaluation where it revealed that the extent of RM distribution from the intranasally administered spanlastics to the brain was comparable to that of the IV drug solution with significantly high brain-targeting efficiency (458.47%). These results suggest that the IN administration of the optimized RM-loaded spanlastics could be a promising, non-invasive alternative for the efficient delivery of RM to brain tissues to exert its pharmacological activities without being dissipated to other body organs which subsequently may result in higher pharmacological efficiency and better safety profile. Graphical Abstract

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Nanomedicine approaches and strategies for gum-based stealth nanocarriers

Bali

Karemore

Jadhav

et al. 2022

Micro- And Nanoengineered Gum-Based Biomaterials for Drug Delivery and Biomedical Applications

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Enhanced transdermal permeation of rasagiline mesylate nanoparticles: design, optimization, and effect of binary combinations of solvent systems across biological membrane

Cited by 10 publications

References 48 publications

Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug’s Solubility Improvement

Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug’s Solubility Improvement

Thin film hydration versus modified spraying technique to fabricate intranasal spanlastic nanovesicles for rasagiline mesylate brain delivery: Characterization, statistical optimization, and in vivo pharmacokinetic evaluation

Nanomedicine approaches and strategies for gum-based stealth nanocarriers

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