Improved dissolution and cytotoxicity of camptothecin incorporated into oxidized-cellulose microspheres prepared by spray drying

Vijay Kumar, Jichao Kang, Raymond J. Hohl

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

Oxidized celluloses (OC) containing 7, 13, and 20% carboxylic content (OC-7, OC-13, and OC-20, respectively) have been converted into aqueous colloidal dispersions and used to prepare microspheres of the antineoplastic agent camptothecin (CPT) by spray drying. Plasticizers used were glycerin, polyethylene glycol 400 (PEG-400), and polyethylene glycol 6000 (PEG-6000). Irrespective of the carboxylic content of OC and the nature of plasticizer employed, the size of microspheres varied from 1.25 ± 0.40 to 1.52 ± 0.47 μm. The release studies in pH 7.4 buffer revealed the dissolution of CPT to be faster from the microsphere formulations than from physical mixtures and free CPT. The times to release 50% CPT (T-50%) from microspheres prepared using OC-7, OC-13, and OC-20 were about 31, 37, and 19 h, respectively. The in vitro cytotoxicity results indicated OC-20/CPT microspheres to be more effective than free CPT against human-derived RPMI-8402 lymphoid and THP-1 myeloid leukemia cell lines. The ED50 values for the OC-20/CPT microspheres and free CPT were 1 × 10-5 and 0.25 × 10-1 μg/mL, respectively, against the RPMI-8402 line and 0.5 × 10-2 and 0.75 μg/mL, respectively, against the THP-1 line. The higher activity of OC-20/CPT microspheres compared to that of the free drug is attributed to increased dissolution of CPT from microspheres.

Original languageEnglish (US)
Pages (from-to)459-467
Number of pages9
JournalPharmaceutical Development and Technology
Volume6
Issue number3
DOIs
StatePublished - Aug 6 2001

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oxidized cellulose
Camptothecin
Microspheres
Plasticizers
Myeloid Leukemia
Myeloid Cells
Antineoplastic Agents
Glycerol

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

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title = "Improved dissolution and cytotoxicity of camptothecin incorporated into oxidized-cellulose microspheres prepared by spray drying",
abstract = "Oxidized celluloses (OC) containing 7, 13, and 20{\%} carboxylic content (OC-7, OC-13, and OC-20, respectively) have been converted into aqueous colloidal dispersions and used to prepare microspheres of the antineoplastic agent camptothecin (CPT) by spray drying. Plasticizers used were glycerin, polyethylene glycol 400 (PEG-400), and polyethylene glycol 6000 (PEG-6000). Irrespective of the carboxylic content of OC and the nature of plasticizer employed, the size of microspheres varied from 1.25 ± 0.40 to 1.52 ± 0.47 μm. The release studies in pH 7.4 buffer revealed the dissolution of CPT to be faster from the microsphere formulations than from physical mixtures and free CPT. The times to release 50{\%} CPT (T-50{\%}) from microspheres prepared using OC-7, OC-13, and OC-20 were about 31, 37, and 19 h, respectively. The in vitro cytotoxicity results indicated OC-20/CPT microspheres to be more effective than free CPT against human-derived RPMI-8402 lymphoid and THP-1 myeloid leukemia cell lines. The ED50 values for the OC-20/CPT microspheres and free CPT were 1 × 10-5 and 0.25 × 10-1 μg/mL, respectively, against the RPMI-8402 line and 0.5 × 10-2 and 0.75 μg/mL, respectively, against the THP-1 line. The higher activity of OC-20/CPT microspheres compared to that of the free drug is attributed to increased dissolution of CPT from microspheres.",
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Improved dissolution and cytotoxicity of camptothecin incorporated into oxidized-cellulose microspheres prepared by spray drying. / Kumar, Vijay; Kang, Jichao; Hohl, Raymond J.

In: Pharmaceutical Development and Technology, Vol. 6, No. 3, 06.08.2001, p. 459-467.

Research output: Contribution to journalArticle

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AU - Kumar, Vijay

AU - Kang, Jichao

AU - Hohl, Raymond J.

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N2 - Oxidized celluloses (OC) containing 7, 13, and 20% carboxylic content (OC-7, OC-13, and OC-20, respectively) have been converted into aqueous colloidal dispersions and used to prepare microspheres of the antineoplastic agent camptothecin (CPT) by spray drying. Plasticizers used were glycerin, polyethylene glycol 400 (PEG-400), and polyethylene glycol 6000 (PEG-6000). Irrespective of the carboxylic content of OC and the nature of plasticizer employed, the size of microspheres varied from 1.25 ± 0.40 to 1.52 ± 0.47 μm. The release studies in pH 7.4 buffer revealed the dissolution of CPT to be faster from the microsphere formulations than from physical mixtures and free CPT. The times to release 50% CPT (T-50%) from microspheres prepared using OC-7, OC-13, and OC-20 were about 31, 37, and 19 h, respectively. The in vitro cytotoxicity results indicated OC-20/CPT microspheres to be more effective than free CPT against human-derived RPMI-8402 lymphoid and THP-1 myeloid leukemia cell lines. The ED50 values for the OC-20/CPT microspheres and free CPT were 1 × 10-5 and 0.25 × 10-1 μg/mL, respectively, against the RPMI-8402 line and 0.5 × 10-2 and 0.75 μg/mL, respectively, against the THP-1 line. The higher activity of OC-20/CPT microspheres compared to that of the free drug is attributed to increased dissolution of CPT from microspheres.

AB - Oxidized celluloses (OC) containing 7, 13, and 20% carboxylic content (OC-7, OC-13, and OC-20, respectively) have been converted into aqueous colloidal dispersions and used to prepare microspheres of the antineoplastic agent camptothecin (CPT) by spray drying. Plasticizers used were glycerin, polyethylene glycol 400 (PEG-400), and polyethylene glycol 6000 (PEG-6000). Irrespective of the carboxylic content of OC and the nature of plasticizer employed, the size of microspheres varied from 1.25 ± 0.40 to 1.52 ± 0.47 μm. The release studies in pH 7.4 buffer revealed the dissolution of CPT to be faster from the microsphere formulations than from physical mixtures and free CPT. The times to release 50% CPT (T-50%) from microspheres prepared using OC-7, OC-13, and OC-20 were about 31, 37, and 19 h, respectively. The in vitro cytotoxicity results indicated OC-20/CPT microspheres to be more effective than free CPT against human-derived RPMI-8402 lymphoid and THP-1 myeloid leukemia cell lines. The ED50 values for the OC-20/CPT microspheres and free CPT were 1 × 10-5 and 0.25 × 10-1 μg/mL, respectively, against the RPMI-8402 line and 0.5 × 10-2 and 0.75 μg/mL, respectively, against the THP-1 line. The higher activity of OC-20/CPT microspheres compared to that of the free drug is attributed to increased dissolution of CPT from microspheres.

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