Formulation development and upscaling of lipid nanocapsules as a drug delivery system for a novel cyclic GMP analogue intended for retinal drug delivery

Urimi, Dileep; Widenbring, Ronja; García, Raúl Oswaldo Pérez; Gedda, Lars; Edwards, Katarina; Loftsson, Þorsteinn; Schipper, Nicolaas

doi:10.1016/j.ijpharm.2021.120640

Cited by 19 publications

(9 citation statements)

References 36 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Unloaded LNCs showed a near zero zeta potential, irrespective of the presence or absence of deuterium. However, similar to earlier results by Urimi et al, 9 upon loading of DF003, LNCs showed a more negative zeta potential of about −10 mV, values that were also independent of deuterium. This increase in negative zeta potential could be attributed to the strong interaction of hydrophilic DF003 with the hydrophilic headgroup region of the amphiphilic surfactant (Kolliphor HS 15).…”

Section: Resultssupporting

confidence: 90%

“… 31 In previous studies, it has also been demonstrated that the LNCs appear very similar with and without drug loading. 9 …”

Section: Resultsmentioning

confidence: 99%

“…In our previous work, we have demonstrated the stability of DF003-loaded LNCs with hyaluronic acid sodium to check for the suitability of LNCs for ocular administration. 9 To further investigate their stability, both unloaded and drug-loaded h-LNCs were diluted with sodium chloride dissolved in D 2 O to a final salt concentration of ∼5 mg/mL and SANS profiles were generated ( Figure 9 ). Scattering profiles remained the same with and without the presence of excess NaCl.…”

Section: Resultsmentioning

confidence: 99%

“…A phase inversion method was employed for preparing LNCs as described by Valcourt et al. 1 and Urimi et al 9 In short, for preparing fully hydrogenated LNCs (h-LNCs), 620 mg of Labrafac, 480 mg of Kolliphor HS 15, 50 mg of sodium chloride, 40 mg of Phospholipon 90 H, and 1.7 mL of purified water/deuterium oxide (D 2 O) were heated to 50 °C until a clear solution was observed. This clear solution was then further heated to 90 °C followed by cooling it to 60 °C.…”

Section: Methodsmentioning

confidence: 99%

See 3 more Smart Citations

Structural Characterization Study of a Lipid Nanocapsule Formulation Intended for Drug Delivery Applications Using Small-Angle Scattering Techniques

et al. 2022

Self Cite

View full text Add to dashboard Cite

Lipid nanocapsules (LNCs) are increasingly being used for various drug delivery applications due to their versatile nature and ability to carry a wide variety of therapeutic drug molecules. In the present investigation, small-angle X-ray (SAXS) and neutron scattering (SANS) techniques were used to elucidate the structure of LNCs. Overall, size measurements obtained from SAXS and SANS techniques were complemented with dynamic light scattering, zeta potential, and cryogenic transmission electron microscopy measurements. The structural aspects of LNCs can be affected by drug loading and the properties of the drug. Here, the impact of drug loading on the overall structure was evaluated using DF003 as a model drug molecule. LNCs with varying compositions were prepared using a phase inversion method. Combined analysis of SAXS and SANS measurements indicated the presence of a core–shell structure in the LNCs. Further, the drug loading did not alter the overall core–shell structure of the LNCs. SANS data revealed that the core size remained unchanged with a radius of 20.0 ± 0.9 nm for unloaded LNCs and 20.2 ± 0.6 nm for drug-loaded LNCs. Furthermore, interestingly, the shell becomes thicker in an order of ∼1 nm in presence of the drug compared to the shell thickness of unloaded LNCs as demonstrated by SAXS data. This can be correlated with the strong association of hydrophilic DF003 with Kolliphor HS 15, a polyethylene glycol-based surfactant that predominantly makes up the shell, resulting in a drug-rich hydrated shell.

show abstract

Section: Resultssupporting

confidence: 90%

“… 31 In previous studies, it has also been demonstrated that the LNCs appear very similar with and without drug loading. 9 …”

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Structural Characterization Study of a Lipid Nanocapsule Formulation Intended for Drug Delivery Applications Using Small-Angle Scattering Techniques

et al. 2022

Self Cite

View full text Add to dashboard Cite

show abstract

“…However, no procedure regarding the formulation of drug-loaded particulate systems has been standardized, although several there are reported as synthetic methods and drug loading techniques. The major developmental issues in the case of particulated systems include particle size uniformity, formulation stability, drug release control rate and manufacturing sterile preparations for large scale systems [ 21 , 22 ]. To increase the efficiency of uptake, certain modifications have been investigated, including conjugation with specific ligands such as thiamine [ 23 ] or transferrine [ 24 ], or coating with surfactant [ 25 ].…”

Section: Introductionmentioning

confidence: 99%

Drug-Loaded Polymeric Particulated Systems for Ophthalmic Drugs Release

et al. 2022

View full text Add to dashboard Cite

Drug delivery to the anterior or posterior segments of the eye is a major challenge due to the protection barriers and removal mechanisms associated with the unique anatomical and physiological nature of the ocular system. The paper presents the preparation and characterization of drug-loaded polymeric particulated systems based on pre-emulsion coated with biodegradable polymers. Low molecular weight biopolymers (chitosan, sodium hyaluronate and heparin sodium) were selected due to their ability to attach polymer chains to the surface of the growing system. The particulated systems with dimensions of 190–270 nm and a zeta potential varying from −37 mV to +24 mV depending on the biopolymer charges have been obtained. Current studies show that particles release drugs (dexamethasone/pilocarpine/bevacizumab) in a safe and effective manner, maintaining therapeutic concentration for a longer period of time. An extensive modeling study was performed in order to evaluate the drug release profile from the prepared systems. In a multifractal paradigm of motion, nonlinear behaviors of a drug delivery system are analyzed in the fractal theory of motion, in order to correlate the drug structure with polymer. Then, the functionality of a SL(2R) type ”hidden symmetry” implies, through a Riccati type gauge, different ”synchronization modes” (period doubling, damped oscillations, quasi-periodicity and intermittency) during the drug release process. Among these, a special mode of Kink type, better reflects the empirical data. The fractal study indicated more complex interactions between the angiogenesis inhibitor Bevacizumab and polymeric structure.

show abstract

Pyruvate-conjugation of PEGylated liposomes for targeted drug delivery to retinal photoreceptors

Christensen

Chen

Urimi

et al. 2023

Biomedicine & Pharmacotherapy

View full text Add to dashboard Cite

Formulation development and upscaling of lipid nanocapsules as a drug delivery system for a novel cyclic GMP analogue intended for retinal drug delivery

Cited by 19 publications

References 36 publications

Structural Characterization Study of a Lipid Nanocapsule Formulation Intended for Drug Delivery Applications Using Small-Angle Scattering Techniques

Structural Characterization Study of a Lipid Nanocapsule Formulation Intended for Drug Delivery Applications Using Small-Angle Scattering Techniques

Drug-Loaded Polymeric Particulated Systems for Ophthalmic Drugs Release

Pyruvate-conjugation of PEGylated liposomes for targeted drug delivery to retinal photoreceptors

Contact Info

Product

Resources

About