Development of Novel Solid Nanostructured Lipid Carriers for Bioavailability Enhancement Using a Quality by Design Approach

Bajwa, Neha; Mahal, Shipra; Naryal, Srishti; Singh, Preet Amol; Baldi, Ashish

doi:10.1208/s12249-022-02386-7

Cited by 11 publications

(2 citation statements)

References 33 publications

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“…Furthermore, robust state properties such as molecule size, internal energy, glasslike or nebulous structure, atomic mobility, and wettability impact the medication's solubility. Using ART-loaded SLNs vs. pure ART [40].…”

Section: Studies On Permeabilitymentioning

confidence: 99%

Implementing Quality by Design (Qbd) Strategy for Optimization of lyophilized Solid Lipid Nanoparticles to Boost Oral Bioavailability of antimalarial drug

Bajwa,

Singh,

Madan

et al. 2024

Preprint

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Background: Arteether (ART) is artemisinin derivatives drug used for resistant malaria. It has oral bioavailability of almost 0.98 %. AIM: ART loaded solid lipid nanoparticles (SLN) were developed with enhanced bioavailability using Quality by Design approach. Methodology: ART loaded SLNs were prepared by solvent emulsification/evaporation method using Quality by Design approach. Surfactant concentration and acetone to ethanol volume ratio were selected as independent variable while particle size and entrapment efficiency was selected as responses using central composite design. Result: The produced SLN were lyophilized and the powdered SLNs was encapsulated in an enteric coated capsule shell. The particle diameters of all the formulations were between 109 and 250 nm, and the entrapment effectiveness was 93.7 %. The XRD spectrum revealed that the ART was in amorphous form. The ART-SLNs release pattern revealed that ART was released in a slow yet time-dependent manner, which seems beneficial to prevent it from acid degradation. The permeability of ART containing formulations was investigated using the Franz diffusion cell technique. The concentration of ART employing ART-SLN to pure ART in the pig's intestine was nearly 7.1 fold enhanced. The pharmacokinetics of ART-SLN administered orally to rabbit models was investigated. The bioavailability of ART-loaded SLN was increased to 27.64%. Conclusion: These findings suggest that formulation development by using quality-by-design in present study also provide a comprehensive solution to develop oral formulation of arteether with desired bioavailability at industrial scale.

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Section: Studies On Permeabilitymentioning

confidence: 99%

Implementing Quality by Design (Qbd) Strategy for Optimization of lyophilized Solid Lipid Nanoparticles to Boost Oral Bioavailability of antimalarial drug

Bajwa,

Singh,

Madan

et al. 2024

Preprint

Self Cite

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“…The effectiveness of the oral administration of the active ingredients and biomolecules depends on the degree of their degradation in the severely acid environment of the stomach. The use of nanoparticles in recent years as a new scientific model has gained significant importance in various fields due to their unique properties, which contribute to the increased involvement of science and technology [24]. Nanomedicine has provided new approaches to improve oral delivery of drugs with poor solubility, low stability and bioavailability, and various administration restrictions [25].…”

Section: Introductionmentioning

confidence: 99%

Safety of Innovative Nanotechnology Oral Formulations Loaded with Bioactive Menopause Molecules: Influence of Genotoxicity and Biochemical Parameters on a Menopausal Rat Model

Crișan,

Pop,

Lacatusu

et al. 2023

Nutrients

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In recent years, nanoparticles have gained significant importance due to their unique properties, such as pharmacological, electrical, optical, and magnetic abilities, contributing to the growth of the science and technology sector. Particular naturally derived biomolecules with beneficial effects on menopause disorder have been the subject of studies of pharmaceutical formulation to obtain alternative pharmaceutical forms with increased bioavailability and without side effects, as in nanostructured lipid carriers (NLCs) loaded with such active ingredients. In the present study, one stage of a broader project, we have performed pharmacotoxicology studies for six combinatory innovative nanocapsule pharmaceutical forms containing active natural biomolecules before considering them as oral formulas for (1) in vitro toxicity studies on culture cells and (2) in vivo preclinical studies on a surgically induced menopause model of Wistar female rats, and the influence of the NLCs on key biochemical parameters: lipid profile (TG, Chol, HDL), glycemic markers (Gli), bone markers (Pac, Palc, Ca, phosphorus), renal markers (Crea, urea, URAC), inflammation (TNF), oxidative stress (GSH, MDA), and estrogen–progesterone hormonal profile. The micronucleus test did not reveal the genotoxicity of the tested compounds; the menopause model showed no significant safety concerns for the six tested formulas evaluated using the blood biochemical parameters; and the results showed the potential hypoglycemic, hypolipidemic, hypouricemic, and antioxidant potential of one of the tested formulas containing nano diosgenin and glycyrrhizic acid.

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Cyclodextrin‐Based Molecular Inclusion by Grinding

Sharma,

Naman,

Baldi

2023

Sustainable Approaches in Pharmaceutical Sciences

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Development of Novel Solid Nanostructured Lipid Carriers for Bioavailability Enhancement Using a Quality by Design Approach

Cited by 11 publications

References 33 publications

Implementing Quality by Design (Qbd) Strategy for Optimization of lyophilized Solid Lipid Nanoparticles to Boost Oral Bioavailability of antimalarial drug

Implementing Quality by Design (Qbd) Strategy for Optimization of lyophilized Solid Lipid Nanoparticles to Boost Oral Bioavailability of antimalarial drug

Safety of Innovative Nanotechnology Oral Formulations Loaded with Bioactive Menopause Molecules: Influence of Genotoxicity and Biochemical Parameters on a Menopausal Rat Model

Cyclodextrin‐Based Molecular Inclusion by Grinding

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