Freeze-dried chitosan/pectin nasal inserts for antipsychotic drug delivery

Luppi, Barbara; Bigucci, Federica; Abruzzo, Angela; Corace, Giuseppe; Cerchiara, Teresa; Zecchi, Vittorio

doi:10.1016/j.ejpb.2010.04.013

Cited by 98 publications

(43 citation statements)

References 18 publications

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“…Drug absorption via the buccal mucosa surface and into the systemic circulation is relatively fast (compared to the skin) owing to the highly vascularized structure underneath the mucosal tissues [1,2].…”

Section: Introductionmentioning

confidence: 99%

Lyophilized wafers comprising carrageenan and pluronic acid for buccal drug delivery using model soluble and insoluble drugs

Kianfar

Antonijević

Chowdhry

et al. 2013

Colloids and Surfaces B: Biointerfaces

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Lyophilized muco-adhesive wafers with optimum drug loading for potential buccal delivery have been developed. A freeze-annealing cycle was used to obtain optimized wafers from aqueous gels containing 2% κ-carrageenan (CAR 911), 4% pluronic acid (F127), 4.4% w/w polyethylene glycol with 1.8% w/w paracetamol or 0.8% w/w ibuprofen. Thermogravimetric analysis showed acceptable water content between 0.9 -1.5%. Differential scanning calorimetry and X-ray diffraction showed amorphous conversion for both drugs. Texture analysis showed ideal mechanical and mucoadhesion characteristics whilst both drugs remained stable over six months and drug dissolution at a salivary pH showed gradual release within two hours. The results show the potential of CAR 911 and F127 based wafers for buccal mucosa drug delivery.Keywords: Amorphous, Buccal drug delivery system, Carrageenan, Dissolution characteristics, Lyophilized wafer, (Muco)-adhesion, 3 IntroductionMucosal drug delivery systems have many advantages such as bypassing first pass liver metabolism and avoiding GI enzymatic degradation. Drug absorption via the buccal mucosa surface and into the systemic circulation is relatively fast (compared to the skin) owing to the highly vascularized structure underneath the mucosal tissues [1,2].Lyophilisation has been used in pharmaceutical industries to improve the stability of formulations. The investigation of fundamental physical phenomena occurring during each step of freeze drying has enabled formulators to produce stable and well-designed freezedried pharmaceutical dosage forms [3]. Freeze dried products do not necessarily need to be refrigerated and can be stored at ambient temperatures. This will be favourable for labile drugs including vaccines and proteins [4].Lyophilisation comprises a freezing step where ice crystals form and the solute becomes extremely concentrated. As the temperature falls below the glass transition temperature (T g ), the system is changed into a viscous glass. Incomplete crystallization may, however, lead to sample collapse or formation of mixtures of different polymorphic forms that causes problems in characterization and manufacturing reproducibility. Frozen products can be categorized as either crystalline or amorphous glass in structure. Crystalline products have a distinct "eutectic" freezing/melting point which is referred to as the collapse temperature. Amorphous products have a corresponding "glass transition" temperature and they are much more difficult to freeze-dry. Even though most materials that are freeze dried are actually amorphous, the term "eutectic" is often used to define the freezing/melting point of sample [4].To optimise the process of solute crystallization during freezing, thermal treatment, or "annealing", will be advantageous. Annealing is the process of heating a sample above its 4 glass transition temperature (but below the eutectic and/or ice melting temperature) and allowing the glass to relax and crystallize. Metastable glass formation is possible depending on the f...

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Section: Introductionmentioning

confidence: 99%

Lyophilized wafers comprising carrageenan and pluronic acid for buccal drug delivery using model soluble and insoluble drugs

Kianfar

Antonijević

Chowdhry

et al. 2013

Colloids and Surfaces B: Biointerfaces

View full text Add to dashboard Cite

show abstract

“…Though the cost of the specialized equipment employed for lyophilisation can be considerably high, it is particularly useful for formulation and storage of thermo-labile products. In addition, lyophilized products do not necessarily need to be refrigerated and can be stored at ambient temperatures 6 .…”

Section: Introductionmentioning

confidence: 99%

Development and physico-mechanical characterization of carrageenan and poloxamer-based lyophilized matrix as a potential buccal drug delivery system

Kianfar

Ayensu

Boateng

2013

Drug Development and Industrial Pharmacy

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“…It was suggested that chitosan/hyaluronate polyelectrolyte complexes can be used for the delivery of peptide and protein drugs as nasal inserts [59]. In a subsequent study Luppi et al [60] investigated the development of chitosan/pectin based chlorpromazine hydrochloride nasal inserts to improve bioavailability of antipsychotic drugs. Chitosan/pectin polyelectrolyte complexes…”

Section: Overview Of Work On Nasal Insertsmentioning

confidence: 99%

“…For the same reason, high percentages of pectin showed the best in vitro mucoadhesion ability which verifies the formation of polyelectrolyte complexes between chitosan and pectin at pH values in the vicinity of the pKa interval of the two polymers. This work has contributed to the understanding of chitosan/pectin polyelectrolyte complex formation and complexation with chlorpromazine hydrochloride and will be furthered by performing intranasal absorption studies in animal models [60].…”

Section: Overview Of Work On Nasal Insertsmentioning

confidence: 99%

“…In the context of the foregoing, nasal delivery studies are few despite its many advantages, probably owing to some limitations. However, studies on nasal inserts of some active molecules and proteins using mucoadhesive polymers such as cellulose derivatives, acrylic acid derivatives, polysaccarides and gums are outlined here [38,[46][47][48][49][50][51][52][53][54][55][56][57][58][59][60][61][62].…”

Section: Overview Of Work On Nasal Insertsmentioning

confidence: 99%

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