Development and in vivo evaluation of functionalized ritonavir proliposomes for lymphatic targeting

Vasif Ahammed, Reema Narayan, John Paul, Yogendra Nayak, Bisakha Roy, Gopal V. Shavi, Usha Y. Nayak

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Aims The aim of the present work was to prepare, characterize, and evaluate proliposomes containing lipophilic prodrug ritonavir for targeting towards CD4 + T cells in the lymphatic system. Materials and methods The liposomes were prepared by lipid thin film hydration method and lyophilized in the presence of cryoprotectant mannitol to obtain proliposomes. The optimized proliposomes by Central Composite Design, were surface modified with biotin. The proliposomes were evaluated for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency, in vitro drug release, in vivo pharmacokinetics and biodistribution studies. Key findings The mean particle size was found to be in the range of 126.6 to 306.2 nm with PDI of 0.340–1.00. The entrapment efficiency was found to be in the range of 18.9 to 86.2%. The formulations showed a zeta potential in the range of − 18.1 to − 20.2 mv. Biotinylated proliposomes (LIP-5B) were in the size of 149.8 ± 6.8 nm with entrapment efficiency 61.6%. The % CDR of pure drug, conventional, biotinylated proliposome in 3 h was found to be 58.3, 82.04, and 95.9% respectively. In vitro drug release and in vivo pharmacokinetics of the pure drug, optimized conventional proliposomes (LIP-5) and biotin proliposomes (LIP-5B) were executed. Significance The AUC for the liposomes were found to be much higher in the spleen and thymus compared to that in the plasma which indicated that the developed formulations enhance the bioavailability and target specificity compared to that of the pure drug thereby enhancing bioavailability at target site.

Original languageEnglish
Pages (from-to)11-20
Number of pages10
JournalLife Sciences
Volume183
DOIs
Publication statusPublished - 15-08-2017

Fingerprint

Ritonavir
Biotin
Particle Size
Liposomes
Biological Availability
Pharmacokinetics
Pharmaceutical Preparations
Polydispersity
Zeta potential
Lymphatic System
Prodrugs
Mannitol
Thymus Gland
Area Under Curve
Particle size
Spleen
Thymus
T-cells
T-Lymphocytes
Lipids

All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Ahammed, Vasif ; Narayan, Reema ; Paul, John ; Nayak, Yogendra ; Roy, Bisakha ; Shavi, Gopal V. ; Nayak, Usha Y. / Development and in vivo evaluation of functionalized ritonavir proliposomes for lymphatic targeting. In: Life Sciences. 2017 ; Vol. 183. pp. 11-20.
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Development and in vivo evaluation of functionalized ritonavir proliposomes for lymphatic targeting. / Ahammed, Vasif; Narayan, Reema; Paul, John; Nayak, Yogendra; Roy, Bisakha; Shavi, Gopal V.; Nayak, Usha Y.

In: Life Sciences, Vol. 183, 15.08.2017, p. 11-20.

Research output: Contribution to journalArticle

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AU - Ahammed, Vasif

AU - Narayan, Reema

AU - Paul, John

AU - Nayak, Yogendra

AU - Roy, Bisakha

AU - Shavi, Gopal V.

AU - Nayak, Usha Y.

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N2 - Aims The aim of the present work was to prepare, characterize, and evaluate proliposomes containing lipophilic prodrug ritonavir for targeting towards CD4 + T cells in the lymphatic system. Materials and methods The liposomes were prepared by lipid thin film hydration method and lyophilized in the presence of cryoprotectant mannitol to obtain proliposomes. The optimized proliposomes by Central Composite Design, were surface modified with biotin. The proliposomes were evaluated for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency, in vitro drug release, in vivo pharmacokinetics and biodistribution studies. Key findings The mean particle size was found to be in the range of 126.6 to 306.2 nm with PDI of 0.340–1.00. The entrapment efficiency was found to be in the range of 18.9 to 86.2%. The formulations showed a zeta potential in the range of − 18.1 to − 20.2 mv. Biotinylated proliposomes (LIP-5B) were in the size of 149.8 ± 6.8 nm with entrapment efficiency 61.6%. The % CDR of pure drug, conventional, biotinylated proliposome in 3 h was found to be 58.3, 82.04, and 95.9% respectively. In vitro drug release and in vivo pharmacokinetics of the pure drug, optimized conventional proliposomes (LIP-5) and biotin proliposomes (LIP-5B) were executed. Significance The AUC for the liposomes were found to be much higher in the spleen and thymus compared to that in the plasma which indicated that the developed formulations enhance the bioavailability and target specificity compared to that of the pure drug thereby enhancing bioavailability at target site.

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