In situ forming implants for periodontitis treatment with improved adhesive properties.

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V (2014-05-17)
M P Do, C Neut, E Delcourt, T Seixas Certo, J Siepmann, F Siepmann
RESUMO

Novel in situ forming implants are presented showing a promising potential to overcome one of the major practical hurdles associated with local periodontitis treatment: limited adhesion to the surrounding tissue, resulting in accidental expulsion of at least parts of the implants from the patients' pockets. This leads to high uncertainties in the systems' residence times at the site of action and in the resulting drug exposure. In the present study, the addition of different types and amounts of plasticizers (acetyltributyl citrate and dibutyl sebacate) as well as of adhesive polymers (e.g., cellulose derivatives such as hydroxypropyl methylcellulose) is shown to allow for a significant increase in the stickiness of poly(lactic-co-glycolic acid)-based implants. The systems are formed in situ from N-methyl pyrrolidone-based liquid formulations. Importantly, at the same time, good plastic deformability of the implants can be provided and desired drug release patterns can be fine-tuned using several formulation tools. The antimicrobial activity of this new type of in situ forming implants, loaded with doxycycline hyclate, was demonstrated using the agar well diffusion method and multiple Streptococcus strains isolated from the oral microflora of patients suffering from periodontitis.

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Sigma-Aldrich
1-Methyl-2-pyrrolidinone, anhydrous, 99.5%
Sigma-Aldrich
Doxycycline hyclate
Sigma-Aldrich
1-Methyl-2-pyrrolidinone, ACS reagent, ≥99.0%
Sigma-Aldrich
Sodium metabisulfite, ReagentPlus®, ≥99%
Sigma-Aldrich
1-Methyl-2-pyrrolidinone, ReagentPlus®, 99%
Sigma-Aldrich
1-Methyl-2-pyrrolidinone, suitable for HPLC, ≥99%
Sigma-Aldrich
1-Methyl-2-pyrrolidinone, biotech. grade, ≥99.7%
Sigma-Aldrich
Sodium metabisulfite, reagent grade, 97%
Supelco
Doxycycline hyclate, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Sodium metabisulfite, puriss. p.a., ACS reagent, reag. Ph. Eur., dry, 98-100.5%
Supelco
Sodium metabisulfite, analytical standard
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Doxycycline hyclate, VETRANAL®, analytical standard
Sigma-Aldrich
Sodium metabisulfite, puriss., meets analytical specification of Ph. Eur., BP, NF, FCC, E223, dry, 97-100.5%
Supelco
Sodium Metabisulfite, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Dibutyl sebacate, ≥97.0% (GC)
Supelco
1-Methyl-2-pyrrolidinone, analytical standard
Doxycycline hyclate, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Sodium metabisulfite, tested according to Ph. Eur.
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DL-Cysteine, technical grade
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Dibutyl sebacate, technical grade
USP
Sodium metabisulfite, United States Pharmacopeia (USP) Reference Standard
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Dibutyl sebacate, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Sodium metabisulfite, anhydrous, free-flowing, Redi-Dri, ReagentPlus®, ≥99%
Supelco
Dibutyl sebacate, analytical standard
Supelco
Dibutyl sebacate, Selectophore, ≥97.0%