In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine Models
This study aimed to develop and assess the long-term stability of drug-loaded solid lipid nanoparticles (SLNs). The SLNs were designed to extend the release profile, overcome the problems of bioavailability and solubility, investigate toxicity, and improve the antischistosomal efficacy of praziquant...
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MDPI AG
2022-08-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/23/16/9485 |
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| author | Tayo A. Adekiya Pradeep Kumar Pierre P. D. Kondiah Philemon Ubanako Yahya E. Choonara |
| author_facet | Tayo A. Adekiya Pradeep Kumar Pierre P. D. Kondiah Philemon Ubanako Yahya E. Choonara |
| author_sort | Tayo A. Adekiya |
| collection | DOAJ |
| description | This study aimed to develop and assess the long-term stability of drug-loaded solid lipid nanoparticles (SLNs). The SLNs were designed to extend the release profile, overcome the problems of bioavailability and solubility, investigate toxicity, and improve the antischistosomal efficacy of praziquantel. The aim was pursued using solvent injection co-homogenization techniques to fabricate SLNs in which Compritol ATO 888 and lecithin were used as lipids, and Pluronic F127 (PF127) was used as a stabilizer. The long-term stability effect of the PF127 as a stabilizer on the SLNs was evaluated. Dynamic light scattering (DLS) was used to determine the particle size, stability, and polydispersity. The morphology of the SLNs was examined through the use of transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The chemical properties, as well as the mechanical, thermal, and crystal behaviours of SLNs were evaluated using FTIR, ElastoSens Bio2, XRPD, DSC, and TGA, respectively. SLNs with PF127 depicted an encapsulation efficiency of 71.63% and a drug loading capacity of 11.46%. The in vitro drug release study for SLNs with PF127 showed a cumulative release of 48.08% for the PZQ within 24 h, with a similar release profile for SLNs’ suspension after 120 days. DLS, ELS, and optical characterization and stability profiling data indicate that the addition of PF127 as the surfactants provided long-term stability for SLNs. In vitro cell viability and in vivo toxicity evaluation signify the safety of SLNs stabilized with PF127. In conclusion, the parasitological data showed that in <i>S. mansoni</i>-infected mice, a single (250 mg/kg) oral dosage of CLPF-SLNs greatly improved PZQ antischistosomal efficacy both two and four weeks post-infection. Thus, the fabricated CLPF-SLNs demonstrated significant efficiency inthe delivery of PZQ, and hence are a promising therapeutic strategy against schistosomiasis. |
| first_indexed | 2024-03-09T09:55:49Z |
| format | Article |
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| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-09T09:55:49Z |
| publishDate | 2022-08-01 |
| publisher | MDPI AG |
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| series | International Journal of Molecular Sciences |
| spelling | doaj.art-e59555baba2048f689158f47046990102023-12-01T23:48:49ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-08-012316948510.3390/ijms23169485In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine ModelsTayo A. Adekiya0Pradeep Kumar1Pierre P. D. Kondiah2Philemon Ubanako3Yahya E. Choonara4Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South AfricaWits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South AfricaWits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South AfricaWits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South AfricaWits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South AfricaThis study aimed to develop and assess the long-term stability of drug-loaded solid lipid nanoparticles (SLNs). The SLNs were designed to extend the release profile, overcome the problems of bioavailability and solubility, investigate toxicity, and improve the antischistosomal efficacy of praziquantel. The aim was pursued using solvent injection co-homogenization techniques to fabricate SLNs in which Compritol ATO 888 and lecithin were used as lipids, and Pluronic F127 (PF127) was used as a stabilizer. The long-term stability effect of the PF127 as a stabilizer on the SLNs was evaluated. Dynamic light scattering (DLS) was used to determine the particle size, stability, and polydispersity. The morphology of the SLNs was examined through the use of transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The chemical properties, as well as the mechanical, thermal, and crystal behaviours of SLNs were evaluated using FTIR, ElastoSens Bio2, XRPD, DSC, and TGA, respectively. SLNs with PF127 depicted an encapsulation efficiency of 71.63% and a drug loading capacity of 11.46%. The in vitro drug release study for SLNs with PF127 showed a cumulative release of 48.08% for the PZQ within 24 h, with a similar release profile for SLNs’ suspension after 120 days. DLS, ELS, and optical characterization and stability profiling data indicate that the addition of PF127 as the surfactants provided long-term stability for SLNs. In vitro cell viability and in vivo toxicity evaluation signify the safety of SLNs stabilized with PF127. In conclusion, the parasitological data showed that in <i>S. mansoni</i>-infected mice, a single (250 mg/kg) oral dosage of CLPF-SLNs greatly improved PZQ antischistosomal efficacy both two and four weeks post-infection. Thus, the fabricated CLPF-SLNs demonstrated significant efficiency inthe delivery of PZQ, and hence are a promising therapeutic strategy against schistosomiasis.https://www.mdpi.com/1422-0067/23/16/9485praziquantelsolid lipid nanoparticlesCompritol ATO 888soy lecithin<i>S. mansoni</i>schistosomiasis |
| spellingShingle | Tayo A. Adekiya Pradeep Kumar Pierre P. D. Kondiah Philemon Ubanako Yahya E. Choonara In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine Models International Journal of Molecular Sciences praziquantel solid lipid nanoparticles Compritol ATO 888 soy lecithin <i>S. mansoni</i> schistosomiasis |
| title | In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine Models |
| title_full | In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine Models |
| title_fullStr | In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine Models |
| title_full_unstemmed | In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine Models |
| title_short | In Vivo Evaluation of Praziquantel-Loaded Solid Lipid Nanoparticles against <i>S. mansoni</i> Infection in Preclinical Murine Models |
| title_sort | in vivo evaluation of praziquantel loaded solid lipid nanoparticles against i s mansoni i infection in preclinical murine models |
| topic | praziquantel solid lipid nanoparticles Compritol ATO 888 soy lecithin <i>S. mansoni</i> schistosomiasis |
| url | https://www.mdpi.com/1422-0067/23/16/9485 |
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