Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats.

Kawakami, Shigeru; Ohshima, Nao; Hirayama, Ryu; Masami, Hirai; Kitahara, Takashi; Sakaeda, Toshiyuki; Mukai, Takahiro; Nishida, Koyo; Nakamura, Junzo; Nakashima, Makoto; Sasaki, Hidetada

doi:10.1248/bpb.25.1072

Cited by 5 publications

(4 citation statements)

References 17 publications

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“…Mice were prepared according to the method reported previously 16,17. Mouse blood was collected and coagulated by incubation for 12 h. After centrifugation (1500 g ) for 10 min, the supernatant was filtered (0.45 µm).…”

Section: Methodsmentioning

confidence: 99%

“…In the present study, the biodistribution characteristics of [ 3 H]ATRA incorporated in liposomes and polymeric micelles (Bz‐75) was investigated after intravenous administration. Because of the lower water solubility of ATRA, it was dissolved in serum to analyze its inherent distribution16,17 [ 3 H] Cholesteryl hexadecyl ether (CHE), which is a cholesterol derivative, was selected as a liposome tracer because of its high lipophilicity 18,19…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Biodistribution characteristics of all-trans retinoic acid incorporated in liposomes and polymeric micelles following intravenous administration

Kawakami

Opanasopit

Yokoyama

et al. 2005

Journal of Pharmaceutical Sciences

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Biodistribution characteristics of all-trans retinoic acid incorporated in liposomes and polymeric micelles following intravenous administration

Kawakami

Opanasopit

Yokoyama

et al. 2005

Journal of Pharmaceutical Sciences

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“…These pharmacokinetic characteristics produced by protein interaction of chol-siRNA corresponds to previous reports that lipophilic prodrugs are distributed following interaction with proteins. [19][20][21][22] Therefore, consideration of the hydrophilic W hydrophobic balance of siRNAs might be one of eŠective approach to enhance their in vivo use.…”

Section: Systemic Delivery Systems Of Sirnasmentioning

confidence: 99%

Targeted Delivery Systems of Small Interfering RNA by Systemic Administration

Kawakami

Hashida

2007

Drug Metabolism and Pharmacokinetics

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RNA interference (RNAi) is induced by 21-25 nucleotide, double-stranded small interfering RNA (siRNA), which is incorporated into the RNAi-induced silencing complex (RISC) and is a guide for cleavage of the complementary target mRNA in the cytoplasm. There are many obstacles to in vivo delivery of siRNAs, such as degradation by enzymes in blood, interaction with blood components and non-specific uptake by the cells, which govern biodistribution in the body. In order to achieve the knockdown by siRNAs in vivo, many delivery systems of siRNAs based on physical and pharmaceutical approaches have been proposed. In addition, the immune responses of siRNA must be taken into account when considering the application of siRNAs to in vivo therapy. This review focuses on recent reports about delivery systems and immune responses of siRNAs.

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“…Dipivefrin showed enhanced corneal penetration with I0 times improved therapeutic index compared to epinephrine [17, 18]. Since then, a plethora of ester prodrugs including adrenergic agonists [19, 20], adrenergic antagonists [21, 22], cholinergics [23, 24], carbonic anhydrase inhibitors [25], prostaglandins [5, 26], antimetabolites [6, 27] and steroids [28, 29] have been prepared and their pharmacokinetic behaviors have been thoroughly explored Ester prodrugs can enhance corneal penetration with improved therapeutic index. However, in some instances these components appear to be chemically instable in aqueous eye drop formulations.…”

Section: Ocular Prodrug Strategiesmentioning

confidence: 99%

Prodrug Strategies in Ocular Drug Delivery

Barot

Bagui²,

Gokulgandhi³

et al. 2012

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Poor bioavailability of topically instilled drug is the major concern in the field of ocular drug delivery. Efflux transporters, static and dynamic ocular barriers often possess rate limiting factors for ocular drug therapy. Different formulation strategies like suspension, ointment, gels, nanoparticles, implants, dendrimers and liposomes have been employed in order to improve drug permeation and retention by evading rate limiting factors at the site of absorption. Chemical modification such as prodrug targeting various nutrient transporters (amino acids, peptide and vitamin) has evolved a great deal ofintereSt to improve ocular drug delivery. In this review, we have discussed various prodrug strategies which have been widely applied for enhancing therapeutic efficacy of ophthalmic drugs. The purpose of this review is to provide an update on the utilization of prodrug concept in ocular drug delivery. In addition, this review will highlight ongoing academic and industrial research and development in terms of ocular prodrug design and delivery.

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Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats.

Cited by 5 publications

References 17 publications

Biodistribution characteristics of all-trans retinoic acid incorporated in liposomes and polymeric micelles following intravenous administration

Biodistribution characteristics of all-trans retinoic acid incorporated in liposomes and polymeric micelles following intravenous administration

Targeted Delivery Systems of Small Interfering RNA by Systemic Administration

Prodrug Strategies in Ocular Drug Delivery

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