Design, Optimization and Characterization of Lamivudine Loaded Solid Lipid Nanoparticles for Targeted Delivery to Brain

Sansare, Vipul; Patel, Nikul G.; Patankar, Neha

doi:10.7897/2230-8407.100258

Cited by 5 publications

(3 citation statements)

References 11 publications

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“…NLCs dispersions were diluted with double distilled water to reduce particle count and better accuracy of results. The resulting diluted dispersions subjected to particle size assessment at 24 °C ( Sansare et al., 2019 ).…”

Section: Methodsmentioning

confidence: 99%

Fabrication and evaluation of mannose decorated curcumin loaded nanostructured lipid carriers for hepatocyte targeting: In vivo hepatoprotective activity in Wistar rats

Gupta

Sansare

Shrivastava

et al. 2022

Current Research in Pharmacology and Drug Discovery

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Curcumin is a well-recognized antioxidant phytoactive isolated from the rhizomes of Curcuma longa . Numerous landmark investigations have proved the antioxidant and hepatoprotective potential of curcumin. The aim of present study was to target curcumin loaded nanocarriers to hepatocytes using asialoglycoprotein receptors targeting strategy. Mannose, a water-soluble carbohydrate, was hydrophobized by anchoring stearylamine with an objective to conjugate mannose on the surface of curcumin loaded nanostructured lipid carriers for targeting asialoglycoprotein receptors on hepatocytes. Mannose conjugated stearylamine was synthesized and characterized using various analytical techniques. The synthesized targeting ligand was incorporated curcumin loaded nanostructured lipid carriers and characterized by photon correlation spectroscopy. Zeta potential measurement was used to confirm the conjugation of the synthesized ligand to the surface of drug-loaded nanostructured lipid carriers. CCl 4 induced hepatotoxicity in male Wistar rats was used as an experimental animal model to evaluate the hepatoprotective potential of formulated drug encapsulated nanostructured lipid carriers. The hepatoprotective potential was assessed by measuring serum liver injury markers and oxidative stress parameters in the liver post–mitochondrial supernatant. Mannose conjugated nanostructured lipid carriers showed acceptable particle size which revealed its suitability for hepatocyte targeting. In addition to this, mannose conjugated nanocarriers revealed significantly better (p < 0.05) reduction of serum liver injury markers and proinflammatory cytokines compared to the unconjugated one which confirmed hepatocytes targeting potential of the synthesized ligand. Asialoglycoprotein receptors targeting could be a landmark strategy for hepatocyte targeting. Thus, the synthesized mannose anchored stearylamine could be a promising novel targeting ligand having hepatocyte targeting potential.

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Section: Methodsmentioning

confidence: 99%

Fabrication and evaluation of mannose decorated curcumin loaded nanostructured lipid carriers for hepatocyte targeting: In vivo hepatoprotective activity in Wistar rats

Gupta

Sansare

Shrivastava

et al. 2022

Current Research in Pharmacology and Drug Discovery

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“…An immensely different drug discharge profile from particles of comparable size based on the same polymer of similar molecular weight demonstrates the significant impact of covalent drug conjugation to the polymeric matrix. Another investigated LV-loaded particle-based DDS included poly(lactic-co-glycolic acid) submicron particles [36], polymethacrylic acid nanoparticles [37], and lipid nanoparticles [38]. All the reported systems released the drug within hours after the introduction to physiological-like conditions.…”

Section: Drug Releasementioning

confidence: 99%

Selected Physicochemical and Pharmaceutical Properties of Poly-ε-caprolactone and Poly(d,l-lactide-co-ε-caprolactone) Conjugates of Lamivudine Synthesized via Ring-Opening Polymerization

Urbaniak

Musiał

2019

Polymers

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The modification of drug fate after administration may be achieved by the covalent coupling of active pharmaceutical ingredients with macromolecules. To prolong or delay the release, slowly degrading polymers such as polyesters may be applied for conjugation. The detachment of a covalently conjugated drug from the polymeric matrix relies mostly on the material degradation profile and barely on the weak interaction between the drug and macromolecules. In the present study, lamivudine was conjugated via ring-opening polymerization with poly-ε-caprolactone and poly(d,l-lactide-co-ε-caprolactone). The influence of the reaction parameters on the course of the polymerization and physicochemical properties of obtained conjugates were investigated. Subsequently, selected reaction products were formulated into submicron particles, and drug release profiles in physiological-like conditions were investigated. The course of the reaction was monitored via gel permeation chromatography. The structure and physicochemical properties of products were evaluated via spectroscopic, calorimetric, and diffractometric methods. The profile of the drug release from particles prepared by the slow evaporation of conjugate solution from o/w emulsion was monitored with high-performance liquid chromatography. Both an elevated reaction temperature and higher catalyst concentration increased the polymerization rate and simultaneously promoted the side reactions, resulting in a broad molecular weight distribution of products in the range from 1.30 to 2.15. The physicochemical properties of conjugates obtained in different conditions varied and had a direct influence on the drug release. The release curve of lamivudine from particles based on low molecular weight conjugates achieved a plateau between 18.9 and 22.2 μg per mg of conjugate within a month. Drug detachment from particles composed of high molecular weight conjugates exhibited a distinct delay period preceded by a drug burst release at a maximal level of 13.3 μg per mg of conjugate. Conjugate chemical composition and the degree of crystallinity were also found to influence the release.

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“…The controlled release is possibly achieved by combining drug with the release modifying polymer. The polymer used to control release of drug from system (Sansare et al, 2019). This could possibly prolong the duration of drug action.…”

Section: Introductionmentioning

confidence: 99%

Design and Evaluation of Natural Mucilage Microspheres of Sesamol for Gastroretentive Drug Delivery

Panda,

Jirole,

Jadhav

et al. 2023

Intern. J. Zool. Invest.

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The mucilages are polysaccharide obtained from various seeds. The mucilage have good swelling and water holding capacity. The mucoadhesive potential of mucilage is recently explored area. Thus, present study aimed to formulate Mimosa pudica mucilage based microspheres for gastroretentive delivery of sesamol. The drug loaded microspheres were formulated using ionic gelation method and evaluated for physicochemical properties, mucoadhesive potential, swelling index and in vitro drug release study. The microspheres showed good particle size and drug entrapment. The good swelling ability, mucoadhesive potential coupled with sustained drug release could be promising for gastroretentive drug delivery. Thus, natural mucilage could be alternative carrier for preparation of mucoadhesive microspheres of drug.

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Design, Optimization and Characterization of Lamivudine Loaded Solid Lipid Nanoparticles for Targeted Delivery to Brain

Cited by 5 publications

References 11 publications

Fabrication and evaluation of mannose decorated curcumin loaded nanostructured lipid carriers for hepatocyte targeting: In vivo hepatoprotective activity in Wistar rats

Fabrication and evaluation of mannose decorated curcumin loaded nanostructured lipid carriers for hepatocyte targeting: In vivo hepatoprotective activity in Wistar rats

Selected Physicochemical and Pharmaceutical Properties of Poly-ε-caprolactone and Poly(d,l-lactide-co-ε-caprolactone) Conjugates of Lamivudine Synthesized via Ring-Opening Polymerization

Design and Evaluation of Natural Mucilage Microspheres of Sesamol for Gastroretentive Drug Delivery

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