Drug Release from Matrix Devices

Cardinal, John R.

doi:10.1007/978-1-4613-2745-5_16

Cited by 13 publications

(4 citation statements)

References 11 publications

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“…A more stringent test was used to distinguish between the mechanisms of drug release. Release data were analyzed accord- ing to the following empirical equation (Higuchi 1963;Cardinal 1984)…”

Section: In Vitro Releasementioning

confidence: 99%

Sodium Alginate Microspheres of Metoprolol Tartrate for Intranasal Systemic Delivery: Development and Evaluation

2003

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Bioadhesive sodium alginate microspheres of Metoprolol tartrate (MT) for intranasal systemic delivery were prepared to avoid the first-pass effect, as an alternative therapy to injection, and to obtain improved therapeutic efficacy in the treatment of hypertension and angina pectoris. The microspheres (Ms) were prepared using emulsification--cross-linking method. The formulation variables were drug loading, polymer concentration, cross-linking agent concentration, and cross-linking time. The Ms were evaluated for characteristics, like particle size, incorporation efficiency, swelling ability, in vitro bioadhesion, in vitro drug release, and in vivo pharmacodynamic performance in rabbits against isoprenaline-induced tachycardia. Treatment of in vitro data to different kinetic equations indicated matrix-diffusion controlled drug delivery from sodium alginate Ms. Polymer concentration, cross-linking agent concentration, and cross-linking time influenced the drug release profiles significantly. In vivo studies indicated significantly improved therapeutic efficacy of MT from Ms with sustained and controlled inhibition of isoprenaline-induced tachycardia as compared with oral and nasal administration of drug solution.

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Section: In Vitro Releasementioning

confidence: 99%

Sodium Alginate Microspheres of Metoprolol Tartrate for Intranasal Systemic Delivery: Development and Evaluation

2003

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“…To examine the drug release kinetics and mechanism, the data were subjected to the following equation (Cardinal 1984):…”

Section: Discussionmentioning

confidence: 99%

“…Initial analysis of drug release data of the formulations supported Higuchi's diffusion controlled release kinetics (Higuchi 1962). To understand the mechanism of diffusioncontrolled release of leuprorelin acetate from leuprorelin acetate formulations, results were analysed according to equation 2 given by Cardinal (1984). High equation coefficient values (a) of leuprorelin acetate and LEU + CS suggested initial burst drug release (Ebube et al 1997).…”

Section: Formulation Equation Coefficient (A) Release Exponent (N)mentioning

confidence: 95%

Preliminary investigation of the nasal delivery of liposomal leuprorelin acetate for contraception in rats

Shahiwala

Misra

2006

Journal of Pharmacy and Pharmacology

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The purpose of the study was to investigate the nasal route as a non-invasive alternative for delivery of leuprorelin acetate (leuprolide acetate, LEU) and to achieve an effective concentration of leuprorelin acetate in blood after nasal administration for contraception in rats. The plain drug solution, physical mixture (plain drug along with constituents of liposomes), or drug encapsulated in either neutral or charged liposomes containing 5 microg leuprorelin acetate were administered to rats through the nasal route. The plain drug solution was administered subcutaneously (s.c.). Simultaneous evaluation was performed on the influence of a mucoadhesive agent (chitosan) on nasal absorption of the plain drug and the liposome-encapsulated drug. Blood samples were taken at regular time intervals and subjected to luteinising hormone (LH) analysis using a specific immunoassay kit. The plasma luteinising hormone concentration vs time data of nasal and subcutaneous treatments were plotted and compared with that of subcutaneous administration. Relative percentage of bioavailability (F) for nasal treatments was calculated from plasma concentration vs time plots. Sperm count and fertility performance studies were carried out for selected formulations in rats. Neutral liposomes (LLEU) and negatively-charged liposomes (LLEUn) showed higher relative percentage of bioavailability (F 27.83 and 21.30%, respectively) as compared with the plain drug and the physical mixture (F 10.89 and 10.96%, respectively) after nasal administration. Hence, work on neutral liposomes was continued. F was further improved after incorporation of chitosan i.e. 10.89 to 49.13% for plain leuprorelin acetate and 27.83 to 88.90% for liposomal leuprorelin acetate formulations. Liposomal chitosan formulation administered nasally and leuprorelin acetate solution subcutaneously achieved complete azoospermia. No implantation sites were observed after the mating of female rats with treated males. It was observed that in the treated female rats, the estrous cycles ceased with the same formulations from the first treatment cycle. The findings of these investigations demonstrated that the bioavailability of the nasally-administered liposomal leuprorelin acetate with chitosan formulation was comparable with that of the subcutaneously administered drug. Complete contraception was obtained in male and female rats that had been treated with either the nasally administered liposomal leuprorelin acetate with chitosan or the subcutaneously administered drug.

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“…An appropriate drug carrier should have high stability, a reasonable lifetime in the systemic circulation, allow for homogeneous distribution of a drug [ 40 ], and release the drug at an anticipated rate. API-ILs have been loaded into mesoporous silica or silica-based ionic gels for controlled drug release [ 37 , 41 ].…”

Section: Introductionmentioning

confidence: 99%

Ionic Liquids as Tools to Incorporate Pharmaceutical Ingredients into Biopolymer-Based Drug Delivery Systems

Bertón

Shamshina

2023

Pharmaceuticals

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This mini-review focuses on the various roles that ionic liquids play in the development and applications of biopolymer-based drug delivery systems (DDSs). Biopolymers are particularly attractive as drug delivery matrices due to their biocompatibility, low immunogenicity, biodegradability, and strength, whereas ILs can assist the formation of drug delivery carriers as 1. dopants to control drug release rate; 2. anchoring agents to incorporate APIs into biopolymeric materials; 3. actives (in the form of API-ILs) for controlled release; or 4. a matrix preparation media.

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Drug Release from Matrix Devices

Cited by 13 publications

References 11 publications

Sodium Alginate Microspheres of Metoprolol Tartrate for Intranasal Systemic Delivery: Development and Evaluation

Sodium Alginate Microspheres of Metoprolol Tartrate for Intranasal Systemic Delivery: Development and Evaluation

Preliminary investigation of the nasal delivery of liposomal leuprorelin acetate for contraception in rats

Ionic Liquids as Tools to Incorporate Pharmaceutical Ingredients into Biopolymer-Based Drug Delivery Systems

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