Development of silicone-based barrier devices for controlled delivery of spermicidal agents

Lee, Chi-Hyun; Bagdon, Robert E.; Bhatt, Padmanabh P.; Chien, Yie W.

doi:10.1016/s0168-3659(96)01499-x

Cited by 10 publications

(9 citation statements)

References 10 publications

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“…To test the intravaginal applicability of FcDDS, the studies were previously conducted utilizing the rabbit and sheep vaginal mucosa. 2 Gel-type FcDDS made from carbopol polymer loaded onto the vagina did not induce any inflammatory response or fibrosis. Subsequently, the next question of whether or not EDTA, which is added as a synergistic agent for the spermicidal activity of sodium dodecyl sulfates (SDS) or Nonoxynol-9 (N-9), has any cytotoxic effects on vaginal mucosa needs to be addressed.…”

Section: Introductionmentioning

confidence: 88%

“…1 The efficiency of FcDDS as a device for fertility control was demonstrated in the animal models, confirming that calcium is one of the regulating factors of sperm, and a removal of calcium by EDTA in semen resulted in reducing sperm motility, consequently affecting the fertilization process. 2 Because biomaterial-induced tissue responses that have no adverse effects are very rare, vaginal mucosa is highly sensitive, and its physiological homeostasis is susceptible to environmental changes, cell-type-specific responses to extracellular stimuli (i.e., the toxic or carcinogenic activity of FcDDS and its components on vaginal mucosa) should be thoroughly monitored. To test the intravaginal applicability of FcDDS, the studies were previously conducted utilizing the rabbit and sheep vaginal mucosa.…”

Section: Introductionmentioning

confidence: 99%

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EDTA‐induced activation of Ca‐regulated proteins in the vaginal mucosa

Choe

Warrier

Chun

et al. 2003

J Biomedical Materials Res

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Abstract:The effects of EDTA on the expression and topologic localization of mitogen-activated protein (MAP) kinases (ERK, JNK, and p38), along with nitric oxide synthase (NOS), I-KappaB, and p53 were examined to elucidate the host response provoked by the intravaginal application of a female controlled drug delivery system (FcDDS) containing a spermicidal/microbicidal agent and EDTA. Immunohistochemical and immunoblotting studies were conducted to identify and quantitate the EDTA-inducible proteins in vaginal mucosa. The content of nitrite, which is one of the primary stable breakdown products of nitric oxide (NO), was determined to correlate the expression of NOS with NO formation in HeLa cervical carcinoma cell line. The immunohistochemical study demonstrated that the modulation of the calcium gradient by EDTA activated MAP kinases (ERK and JNK) in the rabbit vaginal mucosa. The results of Western immunoblot study demonstrated differential expression of MAP kinases (ERK and JNK) with EDTA treatment, whereas the expression of NOS and NF-KappaB was not affected by EDTA. There was no significant difference in nitrite production in the HeLa cell line upon exposure to EDTA compared with the control, which was consistent with the results of the Western blot study. The results of this work support that the regulation of MAP kinase was affected by calcium, which is controlled by chelation activity of EDTA. The specific tissue responses exerted by the loading components of a biomaterial-based system should be fully taken into consideration for its intravaginal application.

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Section: Introductionmentioning

confidence: 88%

Section: Introductionmentioning

confidence: 99%

EDTA‐induced activation of Ca‐regulated proteins in the vaginal mucosa

Choe

Warrier

Chun

et al. 2003

J Biomedical Materials Res

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“…12 Also, there are many papers describing investigations of the controlled release of spermicide using polymeric devices including silicone. [13][14][15][16][17][18] Today in the US and global markets, condoms may be packed dry or with an added lubricant, which may contain N-9 spermicide. There are also many papers dedicated to the industrial application of CD inclusion compounds.…”

Section: Introductionmentioning

confidence: 99%

Nonoxynol‐9‐α‐cyclodextrin inclusion compound and its application for the controlled release of nonoxynol‐9 spermicide

Whang

Hunt

Wrench

et al. 2007

J of Applied Polymer Sci

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Nonoxynol-9 (N-9) is the most active ingredient in commercially available spermicidal products in the United States. There are many applications of cyclodextrin inclusion complexes (CD-ICs), but there are no reported studies investigating the formation of and controlled release from a N-9 spermicide-CD-IC. We have successfully formed the inclusion compound between N-9 and a-CD using a solution-heating technique. The N-9-a-CD-IC was characterized by Fourier Transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, differential scanning calorimetry, thermogravimetric analysis, and wide angle X-ray diffraction observations. Silicone elastomer (SILASTIC MDX4-4210) film embedded with crystalline N-9-a-CD-IC was prepared and evaluated for its efficacy in the controlled release of N-9 spermicide against bovine sperm. Silicone elastomer with N-9-a-CD-IC was as successful in reducing the motility and viability of bovine spermtazoa as silicone elastomer swollen with an equivalent amount of neat N-9. The permeability of the flexible silicone elastomer apparently enables the N-9 spermicide to diffuse from its embedded inclusion complex crystals to contact, immobilize, and kill bovine sperm cells.

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“…In earlier studies, it has been observed (Lee et al, 1997;Roseman, 1972;Kajihara et al, 2003;Chien et al, 1974;Toddywala and Chien, 1990;Malcolm et al, 2003) that polydimethylsiloxane possesses a number of desirable characteristics such as low surface energies, high chain flexibility, stability and non-toxic nature; and it has been widely used for the controlled drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

“…where Q is the accumulated amount of drug released from a unit surface area at time t, D p is the diffusivity of drug across the polymer, C p is the solubility of drug in the polymer matrix, and A is the drug-loading dose (Kim, 2000;Lee et al, 1997). The effect of the In any polymer exposed to radiation, cross-linking and scission occur simultaneously, with different probabilities.…”

Section: Introductionmentioning

confidence: 99%