Zotepine loaded lipid nanoparticles for oral delivery: development, characterization, and in vivo pharmacokinetic studies

Banala, Nagaraj; Tirumalesh, Cernam; Suram, Dinesh; Dudhipala, Narendar

doi:10.1186/s43094-020-00051-z

Cited by 22 publications

(9 citation statements)

References 30 publications

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“…Ex-vivo permeability across the rat intestine revealed a significant enhancement in drug permeability when compared with drug suspension. 40 Likewise, Soni et al found that the prepared lipid nanoparticles that consisted of SA as lipid phase and T-80, capryol 90, and labrasol as surfactants were able to enhance the permeability of Pemetrexed. Ex-vivo permeability study revealed that the developed formulation enhanced the drug permeability ratio by about 6-folds compared to the drug solution.…”

Section: Discussionmentioning

confidence: 99%

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

Sherif¹,

Harisa²,

Alanazi³

et al. 2022

IJN

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Purpose The present study aimed to develop gefitinib-loaded solid lipid nanoparticles (GEF-SLN), and GEF-loaded PEGylated SLN (GEF-P-SLN) for targeting metastatic lung cancer through the lymphatic system. Methods The prepared SLNs were characterized in terms of physicochemical properties, entrapment efficiency, and in-vitro release. Furthermore, ex-vivo permeability was investigated using the rabbit intestine. Cytotoxicity and apoptotic effects were studied against A549 cell lines as a model for lung cancer. Results The present results revealed that the particle size and polydispersity index of the prepared formulations range from 114 to 310 nm and 0.066 to 0.350, respectively, with negative zeta-potential (−14 to −27.6). Additionally, SLN and P-SLN showed remarkable entrapment efficiency above 89% and exhibited sustained-release profiles. The permeability study showed that GEF-SLN and GEF-P-SLN enhanced the permeability of GEF by 1.71 and 2.64-fold, respectively, compared with GEF suspension. Cytotoxicity showed that IC 50 of pure GEF was 3.5 μg/mL, which decreased to 1.95 and 1.8 μg/mL for GEF-SLN and GEF-P-SLN, respectively. Finally, the apoptotic study revealed that GEF-P-SLN decreased the number of living cells from 49.47 to 3.43 when compared with pure GEF. Conclusion These results concluded that GEF-P-SLN is a promising approach to improving the therapeutic outcomes of GEF in the treatment of metastatic lung cancer.

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Section: Discussionmentioning

confidence: 99%

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

Sherif¹,

Harisa²,

Alanazi³

et al. 2022

IJN

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“…To increase the oral bioavailability of zotepine, Nagaraj, et al created Zotepine loaded lipid nanoparticles (ZT-SLN) for oral administration. By freezing the optimised ZT-SLN formulation at or below 80 °C for an extended period of time and lyophilizing it under applied vacuum, the author lyophilized the formulation (Nagaraj et al, 2020).…”

Section: Lyophilizationmentioning

confidence: 99%

Lipid-based oral formulation in capsules to improve the delivery of poorly water-soluble drugs

Mohite,

Singh,

Pawar

et al. 2023

Front. Drug Deliv.

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Poorly water-soluble drugs demonstrate significant challenge in pharmaceutical development, which is linked to their limited oral bioavailability and therapeutic efficacy. To overcome these limitations, lipid-based formulations have emerged as a promising approach to enhance the delivery of such drugs. Moreover, encapsulation within capsules to provide a convenient dosage form for oral administration. The encapsulation techniques are optimized to ensure uniform drug content and efficient encapsulation efficiency. Several investigations demonstrated that the lipid-based formulations in capsules significantly improved the solubility and dissolution rate of poorly water-soluble drugs compared to non-lipid formulations. Additionally, the encapsulation of lipid-based formulations protected the drug against degradation and improved its stability. Overall, incorporating lipid-based formulations in capsules represents a promising strategy for enhancing the delivery of poorly water-soluble drugs with improvement in solubility, dissolution, stability, and bioavailability, overcoming the challenges associated with these challenging drug molecules. The review focussed a brief on utilization of lipids in capsule form to improve therapeutic efficacy of poorly soluble, dissolution and bioavailability of drugs.

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“…The Higuchi model for the release kinetics states that the rate of the release of the drug is a function of the square root of the time [ 41 , 64 ]. Lastly, Korsmeyer–Peppas is a semi-empirical model that can usually be used to describe the mechanism of the drug release phenomenon consisting of diffusion or swelling [ 41 , 65 ].…”

Section: Resultsmentioning

confidence: 99%

Development of α-Tocopherol Succinate-Based Nanostructured Lipid Carriers for Delivery of Paclitaxel

et al. 2022

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The management of retinoblastoma (RB) involves the use of invasive treatment regimens. Paclitaxel (PTX), an effective antineoplastic compound used in the treatment of a wide range of malignant tumors, poses treatment challenges due to systemic toxicity, rapid elimination, and development of resistance. The goal of this work was to develop PTX-loaded, α-tocopherol succinate (αTS)-based, nanostructured lipid carrier (NLCs; αTS-PTX-NLC) and PEGylated αTS-PTX-NLC (αTS-PTX-PEG-NLC) to improve ocular bioavailability. The hot homogenization method was used to prepare the NLCs, and repeated measures ANOVA analysis was used for formulation optimization. αTS-PTX-NLC and αTS-PTX-PEG-NLC had a mean particle size, polydispersity index and zeta potential of 186.2 ± 3.9 nm, 0.17 ± 0.03, −33.2 ± 1.3 mV and 96.2 ± 3.9 nm, 0.27 ± 0.03, −39.15 ± 3.2 mV, respectively. The assay and entrapment efficiency of both formulations was >95.0%. The NLC exhibited a spherical shape, as seen from TEM images. Sterilized (autoclaved) formulations were stable for up to 60 days (last time point checked) under refrigerated conditions. PTX-NLC formulations exhibited an initial burst release and 40% drug release, overall, in 48 h. The formulations exhibited desirable physicochemical properties and could lead to an effective therapeutic option in the management of RB.

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Zotepine loaded lipid nanoparticles for oral delivery: development, characterization, and in vivo pharmacokinetic studies

Cited by 22 publications

References 30 publications

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

PEGylated SLN as a Promising Approach for Lymphatic Delivery of Gefitinib to Lung Cancer

Lipid-based oral formulation in capsules to improve the delivery of poorly water-soluble drugs

Development of α-Tocopherol Succinate-Based Nanostructured Lipid Carriers for Delivery of Paclitaxel

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