The concept of ocular inserts as drug delivery systems: An overview
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Abstract
transition from an empirical to rational basis. In the recent years, there has been explosion of interest in the polymer based delivery devices. Utilization of the principles of controlled release as embodied by ocular inserts offers an attractive
approach to the problem of prolonging pre-corneal drug residence times. In the present update, the authors discuss the basic concept of ocular inserts as drug delivery system and examine the few inserts, which are available in the market or are being developed by pharmaceutical companies for drug delivery.The article discusses soluble ocular drug insert (SODI), Ocusert, Collagen Shields, Ocufit, Minidisc and new ophthalmic delivery system (NODS) with special attention to biological/clinical performances, and potential for future applications and developments.
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References
Chien YW. Ocular drug delivery and delivery systems. In: Novel drug
delivery systems. 2nd ed. New York: Marcel Dekker; 1992. p. 269-70.
Saettone MF, Salminen L. Ocular inserts for topical delivery. Adv Drug
Del Rev 1995;16:95-106.
Khar RK, Vyas SP. Targeted and Controlled drug delivery novel carrier
systems. 1st ed. New Delhi; CBS Publishers and Distributors; 2002.
p. 384.
Gurtler F, Gurny R. Patent literature review of ophthalmic inserts. Drug
Dev Ind Pharm 1995;21:1-18.
Saettone MF. Solid polymeric inserts/disks as ocular drug delivery
systems. In: Edman P, editor. Biopharmaceutics of ocular drug delivery.
Boca Raton: CRC Press; 1993. p. 61-79.
Quigley HA, Pollack IP, Harbin TS Jr. Pilocarpine ocuserts: Long term
clinical trials and selected pharmacodynamics. Arch Ophthalmol
;93:771-5.
Bloomfield SE, Miyata T, Dunn MW, Bueser N, Stenzel KH, Rubin AL.
Soluble artificial tear inserts. Arch Ophthalmol 1977;95:247-50.
Bloomfield SE, Miyata T, Dunn MW, Bueser N, Stenzel KH, Rubin AL.
Soluble gentamicin ophthalmic inserts as a drug delivery system. Arch
Ophthalmol 1978;96:885-7.
Khromow GL, Davydov AB, Maychuk YF, Tishina IF. Base for
ophthalmological medicinal preparations and an ophthalmological
medicinal film. US. Patent 3, 935, 303, 1976.
Maichuk YF. Medicated eye films. Moscow: Med Export; 1985. p.
-66.
Maichuk YF. Polymeric ophthalmic inserts with antibiotics, Proceedings
of the Conference of Ophthalmologists of the City of Moscow; 1967.
p. 403-5.
Lloyd R. U.K. Patent 2097680. Smith and Nephew Research, Ltd;
Milani JK, Verbukh I, Pleyer U, Sumner H, Adamu SA, Halabi HP, et al.
Collagen shields impregnated with gentamicin-dexamethasone as
potential drug delivery device. Am J Ophthalmol 1993;116:622-7.
Wentworth JS, Paterson CA, Wells JT, Tilki N, Gray RS, McCartney MD.
Collagen shields exacerbate ulceration of alkali-burned rabbit corneas.
Arch Ophthalmol 1993;111:389-92.
Kaufman HE, Steinemann TL, Lehman E, Thompson HW, Varnell ED,
Jacob-LaBarre JT, et al. Collagen-based drug delivery and artificial tears.
J Ocul Pharmacol 1994;10:17-27.
Darougar S. Ocular insert for the fornix, U.S. Patent 5,147, 1992,647.
Katz IM, Blackman WM. A soluble sustained-release ophthalmic delivery
unit. Am J Ophthalmol 1977;83:728-34.
Lamberts DW, Pavan-Langston D, Chu W. A clinical study of slow-
releasing artificial tears. Ophthalmology 1978;85:794-800.
Bawa R, Dais M, Nandu M, Robinson JR. New extended release ocular
drug delivery system: Design, characterization and performance
testing of minidisc inserts. Proc Int Symp Control Rel Bioact Mater
;15:106a-b.
Bawa R, Nandu M, Downie W, Robinson JR. Recent studies on the
continuing characterization of minidisc inserts for ocular therapy. Proc
Intern Symp Control Rel Bioact Mater 1989;16:213-4.
Bawa R. Ocular inserts. In: Mitra AK, editor. Ophthalmic Drug Delivery
Systems. New York: Marcel Dekker; 1993. p. 223-59.
Richardson MC, Bentley PH. A new ophthalmic delivery system. In:
Mitra AK, editor. Ophthalmic drug delivery systems. New York: Marcel
Dekker; 1993. p. 355-67.
Kelly J, Molyneux PD, Smith SA, Smith S. Relative bioavailability of
pilocarpine from a novel ophthalmic delivery system and conventional
eye drop formulations. Br J Ophthalmol 1989;7:360-2.
Greaves JL, Wilson CG, Birmingham AT, Bentley PH, Richardson MC.
Scintigraphic studies on the cornea 1 residence of a new ophthalmic
delivery system (NODS): Rate of clearance of a soluble marker in
relation to duration of pharmacological action of pilocarpine. Br J Clin
Pharmacol 1992;33:603-7.
Gurtler F, Kaltsatos V, Boisrame B, Gurny R. Long acting soluble
bioadhesive ophthalmic drug insert (BODI) containing gentamicin for
veterinary use: optimization and clinical investigation. J Control Rel
;33:231-6.
Chetoni P, Di Colo G, Gandi M, Morelli M, Saettone MF, Darougar S.
Silicone rubber/hydrogel composite ophthalmic inserts: Preparation
and preliminary in vitro/in vivo evaluation. Eur J Pharma Biopharm
;46:125-32.
Simamora P, Nadkarni SR, Lee YC, Yalkowsky SH. Controlled delivery
of pilocarpine.2. In vivo evaluation of Gelfoam device. Int J Pharm
;170:209-14.
Diestelhorst M, Grunthal S, Suverkrup R. Dry drops: A new preservative-
free drug delivery system. Graefes Arch Clin Exp Ophthalmol
;237:394-8.
Urquhart J. Development of the Ocusert pilocarpine ocular therapeutic
systems: A case history in ophthalmic product development. In:
Robinson JR, editor. Ophthalmic Drug Delivery Systems, American
Pharmaceutical Association, Washington DC: 1980. p. 105-16.
Hornof M, Weyenberg W, Ludwig A, Bernkop-Schnurch A. Mucoadhesive
ocular insert based on thiolated poly(acrylic acid): Development and in
vivo evaluation in humans. J Controlled Release 2003;89:419-28.
Sasaki H, Nagano T, Sakanaka K, Kawakami S, Nishida K, Nakamura J, et
al. One-side-coated insert as a unique ophthalmic drug delivery system.
J Controlled Release 2003;92:241-7.
Korsmeyer RW, Peppas NA. Macromolecular and modeling aspects of
swelling-controlled systems. In: Roseman TJ, Mansdorf SZ, editors.
Controlled Release Delivery Systems. New York: Marcel Dekker; 1983.
p. 77-90.
Darougar; Sohrab, Darougar and Dayshad, Patent literature review
of ocular inserts. United States Patent 6,264,971, Appl. No. 428967,
Filed on November 4, 1999.
Heller J. Controlled release of biologically active compounds from
bioerodible polymers. Biomaterials 1980;1:51-7.
Heller J. Controlled drug release from monolithic systems. In:
Saettone MF, Bucci G, Speiser P, editors. Ophthalmic Drug Delivery,
Biopharmaceutical, Technological and Clinical Aspects, Fidia Research
Sereis. Vol. 11. Padua: Liviana Press; 1987. p. 179-89.
Refojo MF. Polymers in contact lenses: An overview. Curr Eye Res
;4:719-23.
Moddox YF, Bernstein HN. An evoluation of the bionite hydrophilic
contact lens for use in a ocular drug delivery system. Ann Ophthalmol
;4:789.
Prans R, Brettschneider, Krjci L, Kahvodova. Hydrophilic contact lenses
as a new therapeutic approach for the typical use of chloramphenicol
and tetracycline. Opthalmologica 1972;165:62.
Hull DS, Edechauser HF, Hyndink RA. Ocular penetration of prednisolone and the hydrophilic contact lense Arch Ophthalmol 1974;92:413.
Saettone MF, Chetoni P, Torraca MT, Giannaccini B, Naber L, Conte U,
et al. Application of the compression technique to the manufacture of
Pilocarpine inserts. Acta Pharm Technol 1990;36:15-9.
Saettone MF, Torraca MT, Pagano A, Giannaccini B, Rodriguez L, Cini M.
Controlled release of Pilocarpine from coated polymeric ophthalmic
inserts prepared by extrusion. Int J Pharm 1992;86:159.
Attia MA, Kassem MA, Safwat SM. In vivo per formance of 3-H-
dexamethasone ophthalmic film delivery system in the Rabbit eye. Int
J Pharm 1988;47:21.
Lee VH, Yong Li S, Sasaki H, Saettone MF, Chetoni P. Influence of drug
release rate on systemic timolol absorption from polymeric ocular
inserts in the pigmented rabbit. J Ocular Pharmacol 1994;10:421-9.
Grass GM, Cobby J, Makoid MC. Ocular delivery of Pilocarpine from
erodible matrices. J Pharm Sci 1984;73:618-21.
Punch PI, Slatter DH, Costa ND, Edwards ME. Investigation of gelatin as a possible biodegradable matrix for Sustained delivery of gentamicin
to the bovine eye. J Vet Pharmacol Ther 1985;8:335-8.
Salminen L, Urtti A, Kujari H, Juslin M. Prolonged pulse-entry of
pilocarpine with a soluble drug insert. Greafe’s Arch Clin Exp
Ophthalmol 1983;221:96.
Saettone MF, Chetoni P, Torraca MT, Burgalassi S, Giannaccini
B. Evaluation of muco- adhesive properties and in vivo activity
of ophthalmic vehicles based on hyaluronic acid. Int J Pharm
;51:203.
Urtti A, Salminen L, Miinalainen O. Systemic absorption of
ocular pilocarpine is modified by polymer matrices. Int J Pharm
;23:147.
Sendelbeck L, Moore D, Urqhart J. Comparative distribution of
pilocarpine in ocular tissues of the rabbit during administration by
eyedrop or by membrane-controlled delivery systems. Am J Ophthalmol
;80:274-83.
Yamamoto Y, Kaga Y, Yoshikawa T, Moribe A. Ultra violet-hardenable
adhesive. US Patent. 5145884 , 1992.
Milani JK, Verbukh I, Pleyer U, Sumner H, Adamu SA, Halabi HP, et al.
Collagen shields impregnated with gentaminic-dexamethasone as a
potential drug delivery device. Am J Ophthalmol 1993;116:622-7.
Pavan-Langston D, Langston RH, Geary PA. Idoxuridine ocular insert
therapy: Use in treatment of experimental herpes simplex keratitis.
Arch Ophthalmol 1975;93:1349.
Rastogi SK, Vaya N, Mishra B. Ophthamic inserts: An overview. The
Eastern Pharmacist, February 1996. p. 41-4.
Hiratani H, Fujiwara A, Tamiya Y, Mizutani Y, Alvarez-Lorenzo C. Ocular
release of Timolol from molecularly imprinted soft contact lenses.
Biomaterials 2005;26:1293-8.
Stephane M, Isabelle M, Belkacem H, Marie-Jose S, Patrick B, Yves T, et al. Pharmacodynamics of a new ophthalmic mydriatic insert in healthy
volunteers: Potential alternative as drug delivery system Prior to cataract
surgery, basic and clinical. Pharmacol Toxicol 2006;98:547-54.
Natu MV, Sardinha JP, Correia IJ, Gil MH. Controlled release gelatin
hydrogels and lyophilisates with potential application as ocular inserts.
Biomed Mater 2007;2:241-9.
Pijls RT, Lindemann S, Nuijts RM, Daube GW, Koole LH. Pradofloxacin
release from the OphthaCoil: A new device for sustained delivery of
drugs to the eye. J Drug Deliv Sci Technol 2007;17:87-91.