Development of ritonavir solid lipid nanoparticles by Box Behnken design for intestinal lymphatic targeting

Kumar, S.L. Hari; Narayan, Reema; Ahammed, Vasif; Nayak, Yogendra; Naha, Anup; Nayak, Usha Yogendra

doi:10.1016/j.jddst.2017.12.014

Cited by 43 publications

(19 citation statements)

References 18 publications

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“…The polydispersity index (PDI) was narrow for all the batches with values of 0.29 ± 0.05, indicating a homogeneous particle size distribution. These results show a smaller particle size and PDI than those reported by Martinez-Acevedo et al [ 24 ] for Compritol ® 888 ATO SLN using polyvinyl alcohol as the stabilizer and the hot dispersion method, and are consistent with those reported by Swapnil-Kumar et al [ 25 ] for Compritol ® 888 ATO SLN loaded with ritonavir and prepared by the solvent evaporation method.…”

Section: Resultssupporting

confidence: 91%

Preparation of Co-Processed Excipients for Controlled-Release of Drugs Assembled with Solid Lipid Nanoparticles and Direct Compression Materials

et al. 2021

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The purpose of the study was to develop a novel, directly compressible, co-processed excipient capable of providing a controlled-release drug system for the pharmaceutical industry. A co-processed powder was formed by adsorption of solid lipid nanoparticles (SLN) as a controlled-release film onto a functional excipient, in this case, dicalcium phosphate dihydrate (DPD), for direct compression (Di-Tab®). The co-processed excipient has advantages: easy to implement; solvent-free; industrial scaling-up; good rheological and compressibility properties; and the capability to form an inert platform. Six different batches of Di-Tab®:SLN weight ratios were prepared (4:0.6, 3:0.6, 2:0.6, 1:0.6, 0.5:0.6, and 0.25:0.6). BCS class III ranitidine hydrochloride was selected as a drug model to evaluate the mixture’s controlled-release capabilities. The co-processed excipients were characterized in terms of powder rheology and dissolution rate. The best Di-Tab®:SLN ratio proved to be 2:0.6, as it showed high functionality with good flow and compressibility properties (Carr Index = 16 ± 1, Hausner Index = 1.19 ± 0.04). This ratio could control release for up to 8 h, so it fits the ideal profile calculated based on biopharmaceutical data. The compressed systems obtained using this powder mixture behave as a matrix platform in which Fickian diffusion governs the release. The Higuchi model can explain their behavior.

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Section: Resultssupporting

confidence: 91%

Preparation of Co-Processed Excipients for Controlled-Release of Drugs Assembled with Solid Lipid Nanoparticles and Direct Compression Materials

et al. 2021

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“…Among other viruses, the human immunodeficiency virus (HIV) mainly proliferates inside macrophages and attacks CD4+ T cells in the lymphatic system (Fevrier, Dorgham, & Rebollo, 2011;Vidya Vijayan, Karthigeyan, Tripathi, & Hanna, 2017). It is challenging for systemically administered anti-retroviral drugs to these reach reservoir sites, causing continuous viral proliferation with poor outcomes for patients (Kumar S., 2018). Therefore, there is a need to develop nanocarriers that are able to deliver antiviral drugs to lymphatic organs.…”

Section: Lym Phatic Deliverymentioning

confidence: 99%

“…Therefore, there is a need to develop nanocarriers that are able to deliver antiviral drugs to lymphatic organs. SLNs are stable drug delivery vehicles that can be orally administered, as they resist gastric acidity (Kumar S., 2018) and are taken up by the intestinal lymphatic system that transports lipids and nanosized particle from the gut into systemic blood circulation (Singh, Swami, Khan, & Sistla, 2014). In rats, it has been shown that orally administered poorly water-soluble antiretroviral drugs encapsulated into SLNs accumulate in lymphatic organs (spleen and thymus).…”

Section: Lym Phatic Deliverymentioning

confidence: 99%

Organotropic drug delivery: Synthetic nanoparticles and extracellular vesicles

Busatto

Pham

Suh

et al. 2019

Biomed Microdevices

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Most clinically approved drugs (primarily small molecules or antibodies) are rapidly cleared from circulation and distribute throughout the body. As a consequence, only a small portion of the dose accumulates at the target site, leading to low efficacy and adverse side effects. Therefore, new delivery strategies are necessary to increase organ and tissue-specific delivery of therapeutic agents. Nanoparticles provide a promising approach for prolonging the circulation time and improving the biodistribution of drugs. However, nanoparticles display several limitations, such as clearance by the immune systems and impaired diffusion in the tissue microenvironment. To overcome common nanoparticle limitations various functionalization and targeting strategies have been proposed. This review will discuss synthetic nanoparticle and extracellular vesicle delivery strategies that exploit organ-specific features to enhance drug accumulation at the target site.

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“…According to the RSM analysis, the F value for the particle size was determined as 376.83 (p = 0.003 <0.05). The F value demonstrated that the selected quadratic model holds significance [20,21]. The coefficient determinant (R 2 ) value was found 94.19% value indicates the reliability of the model together with adjusted R 2 value.…”

Section: Resultsmentioning

confidence: 89%

“…Box-Behnken design can also perform statistical analysis of the model, response optimization, and prediction of the formulations that meet the desired conditions [20,21]. In this study, we used a factorial design for scanning microemulsion components and optimizing SLN formulation.…”

Section: Original Articlementioning

confidence: 99%

Optimization and screening of solid lipid nanoparticle production for gene delivery by factorial design and response surface methodology

Akbaba¹,

Ozder²

2021

j-ebr

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A successful gene therapy requires a delivery system for overcoming various biological barriers. For this, we adapted the factorial design and response surface methodology to the cationic solid lipid nanoparticle production process. Methods: Screening and optimization of formulations were carried out with factorial design with 3 factors and 3 levels using Box-Behnken Design. Then, solid lipid nanoparticles were physicochemically characterized. Furthermore, optimal SLN formulation is examined in terms of complex formation with plasmid DNA, its protection potential against nucleases, cytotoxicity profile, and storage stability. Results: Response-surface analyses demonstrated that the selected quadratic model holds significance for particle size and zeta potential. The interaction of independent variables was statistically determined. Optimization and prediction were performed using obtained second-order polynomial equations. Optimal formulation and complexes were found to be nanosized, positively charged and their polydispersity-index values below 0.3 as an indicator of being monodispersed. Cytotoxicity of the optimal formulation is compatible for further studies and no significant increase was observed in particle size until day 21 and until day 60 for polydispersity-index. Conclusion:Optimal formulation provides a good basis as a gene delivery system was produced with developed systematic. Briefly, this methodology could be used to obtain SLNs with desired conditions.

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Development of ritonavir solid lipid nanoparticles by Box Behnken design for intestinal lymphatic targeting

Cited by 43 publications

References 18 publications

Preparation of Co-Processed Excipients for Controlled-Release of Drugs Assembled with Solid Lipid Nanoparticles and Direct Compression Materials

Preparation of Co-Processed Excipients for Controlled-Release of Drugs Assembled with Solid Lipid Nanoparticles and Direct Compression Materials

Organotropic drug delivery: Synthetic nanoparticles and extracellular vesicles

Optimization and screening of solid lipid nanoparticle production for gene delivery by factorial design and response surface methodology

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