Controlled release of the LHRH agonist buserelin acetate from injectable suspensions containing triacetylated cyclodextrins in an oil vehicle

Matsubara, Kazutaka; Irie, Tetsumi; Uekama, Kaneto

doi:10.1016/0168-3659(94)00030-1

Cited by 14 publications

(6 citation statements)

References 21 publications

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“…First, a simultaneous use of different CDs will enhance the function of each host molecule. 21,28 In particular, the multifunctional characteristics of peracylated or regioselectively acylated CDs may have broad applicability, and they can serve as novel hydrophobic or amphiphilic carriers in various pharmaceutical dosage forms in the near future. 65,70,77,149,197,198 Second, hydrophobic CDs will be useful in various controlled-release formulations of water-soluble drugs including peptide and protein drugs.…”

Section: Resultsmentioning

confidence: 99%

“…28 Both TA-CDs were degraded enzymatically in the rat skin homogenates to give the parent CDs; the residual amounts of TA--CD and TA-γ-CD were 72.4 and 59.9%, respectively, after an 8-h incubation. For instance, heptakis(2,3,6tri-O-acetyl)--CD (TA--CD) and octakis(2,3,6-tri-O-acetyl)γ-CD (TA-γ-CD) have potential for use as bioabsorbable sustained-release carriers for buserelin acetate, a luteinizing hormone-releasing hormone agonist, following the subcutaneous injection of an oily suspension in rats.…”

Section: Introductionmentioning

confidence: 91%

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Pharmaceutical Applications of Cyclodextrins. III. Toxicological Issues and Safety Evaluation

Irie

Uekama

1997

Journal of Pharmaceutical Sciences

835

520

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The objective of this review is to summarize recent findings on the safety profiles of three natural cyclodextrins (alpha-, beta- and gamma-CDs) and several chemically modified CDs. To demonstrate the potential of CDs in pharmaceutical formulations, their stability against non-enzymatic and enzymatic degradations in various body fluids and tissue homogenates and their pharmacokinetics via parenteral, oral, transmucosal, and dermal routes of administration are outlined. Furthermore, the bioadaptabilities of CDs, including in vitro cellular interactions and in vivo safety profiles, via a variety of administration routes are addressed. Finally, the therapeutic potentials of CDs are discussed on the basis of their ability to interact with various endogenous and exogenous lipophiles or, especially for sulfated CDs, their effects on cellular processes mediated by heparin binding growth factors.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 91%

Pharmaceutical Applications of Cyclodextrins. III. Toxicological Issues and Safety Evaluation

Irie

Uekama

1997

Journal of Pharmaceutical Sciences

835

520

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“…Uekama et al 92 and Matsubara et al 93 studied the release after im administration of the LHRH agonist buserelin acetate from oily suspensions in the presence of various cyclodextrins. The effects of HP--CD in altering the activity of a number of opioids and model drugs after intracerebral, intrathecal, and epidural administration have been mixed.…”

Section: Parenteral Applications Of Cyclodextrinsmentioning

confidence: 99%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

759

374

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The objective of this Review is to summarize and critique recent findings and applications of both unmodified and modified cyclodextrins for in vivo drug delivery. This review focuses on the use of cyclodextrins for parenteral, oral, ophthalmic, and nasal drug delivery. Other routes including dermal, rectal, and pulmonary delivery are also briefly addressed. This Review primarily focuses on newer findings concerning cyclodextrin derivatives which are likely to receive regulatory acceptance due to improved aqueous solubility and safety profiles as compared to the unmodified cyclodextrins. Many of the applications reviewed involve the use of hydroxypropyl-beta-cyclodextrins (HP-beta-CDs) and sulfobutylether-beta-cyclodextrins (SBE-beta-CDs) which show promise of greater safety while maintaining the ability to form inclusion complexes. The advantages and limitations of HP-beta-CD, SBE-beta-CD, and other cyclodextrins are addressed.

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“…171) Then, the possible use of bioadaptable per-O-acetylated CyDs (TA-CyDs) as sustained release carriers was studied, since the release of buserelin from the peanut oil suspension into the aqueous phase was significantly retarded by the addition of TA-CyDs. 40) A single subcutaneous injection of the oily suspension of buserelin containing TA-b-CyD or TA-g-CyD in rats enhanced the retardation of plasma buserelin levels, giving 25 and 30 times longer mean residence times, respectively, than that with buserelin alone. Simultaneously, the suppression of plasma testosterone levels to induce castration, the pharmacological effect of buserelin, continued for 1 to 2 weeks and significant weight reduction in genital organs was observed due to the antigonadal effect.…”

Section: Sustained-release Of Peptide and Protein Drugsmentioning

confidence: 99%