Design of In Situ Dispersible and Calcium Cross-Linked Alginate Pellets as Intestinal-Specific Drug Carrier by Melt Pelletization Technique

Harjoh, Nurulaini; Wong, Tin Wui

doi:10.1002/jps.22459

Cited by 19 publications

(6 citation statements)

References 25 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Ten beads of each formulation had their individual length and width measured using the digital caliper and their respective weight characterized. 32 Each bead was then placed in 5 mL of pH 1.2 buffer to simulate gastric conditions and shaken at 50 rpm and 37 °C for 2 h. The weight and size of each wet bead were subsequently measured after removing the surface moisture, achieved by rolling the bead gently over a dry Petri dish until there was no sign of moisture left in its immediate trail on the dish surface. The bead was then oven-dried at 40 °C for 24 h and subsequently equilibrated to a constant weight by storing in a desiccator at 25 °C.…”

Section: Molecular Pharmaceuticsmentioning

confidence: 99%

Alginate–C18 Conjugate Nanoparticles Loaded in Tripolyphosphate-Cross-Linked Chitosan–Oleic Acid Conjugate-Coated Calcium Alginate Beads as Oral Insulin Carrier

2018

Self Cite

View full text Add to dashboard Cite

Simple alginate, alginate-stearic acid, and alginate-C18 conjugate nanoparticles and tripolyphosphate-cross-linked chitosan-oleic acid conjugate-coated calcium alginate beads as the vehicle of nanoparticles were designed. Their size, ζ potential, morphology, drug load, drug release, matrix molecular characteristics, mucus penetration, HT-29 cell line cytotoxicity and intracellular trafficking, in vivo blood glucose lowering, and insulin delivery profiles were characterized. Alginate-C18 conjugate nanoparticles were nontoxic. Among all nanoparticle variants, they had reduced size and ζ potential thus enhancing particulate mucus penetration and intracellular trafficking. Their insulin reabsorption tendency was minimized as alginate active COOH/COO- sites were preoccupied with C18. Their loading into coated beads was translated to reduced drug release in simulated gastric phase with nanoparticles being released in the intestinal phase. The combination dosage form increased the blood glucose lowering extent of insulin and blood insulin level compared with nanoparticles or beads alone. Nanoparticles in beads represented a viable approach for oral insulin delivery.

show abstract

Section: Molecular Pharmaceuticsmentioning

confidence: 99%

Alginate–C18 Conjugate Nanoparticles Loaded in Tripolyphosphate-Cross-Linked Chitosan–Oleic Acid Conjugate-Coated Calcium Alginate Beads as Oral Insulin Carrier

2018

Self Cite

View full text Add to dashboard Cite

show abstract

“…Melt agglomeration refers to solid particle binding by a molten liquid into granules or pellets under agitation forces, usually in a high shear mixer [69,70]. It may be carried out by spray-on or melt-in procedure.…”

Section: Melt Agglomerationmentioning

confidence: 99%

Oral Fast-Release Solid Dispersion-Paradigm Shift to Nanoparticles

Wong

2011

DDF

View full text Add to dashboard Cite

Design of oral fast-release solid dispersion of poorly water-soluble drugs has been a great challenge over past decades on issues of drug recrystallization, drug polymorphism, formulation limited to low drug-to-carrier ratio and drug particle aggregation in matrix. The complexity in solid dispersion design is envisaged to be resolvable by the use of nanoparticulate system as solid dosage form. This manuscript reviews several patented processing approaches of nanoparticulate solid dispersion that have been reported recently. Through drug nanoencapsulation, a higher content of drug may be delivered with less aggregation via placing the same drug mass in a greater number of tinier carriers. Nanoencapsulation, by its own process of formation, brings about submicron particles. Keeping drug in these nanoparticles, a remarkable rise in specific surface area of drug is realized for dissolution. The augmentation of drug dissolution can be sufficiently high to the extent that the influences of polymorphism and crystallization phenomenon on drug dissolution in a solid dispersion may be negligible.

show abstract

“…Chitosan and Ca 2+ have received widespread use as a coacervating polyelectrolyte and crosslinking agent, respectively, in the formulation of oral alginate matrices (Table 1). [38,42,115] Most oral alginate formulations employ Ca 2+ to shape and strengthen the matrices. The addition of chitosan to the calcium alginate matrix enhances its controlled drug release property.…”

Section: Oral Drug Deliverymentioning

confidence: 99%

Alginate graft copolymers and alginate–co-excipient physical mixture in oral drug delivery

Wong

2011

Journal of Pharmacy and Pharmacology

Self Cite

View full text Add to dashboard Cite

Objectives Use of alginate graft copolymers in oral drug delivery reduces dosage form manufacture complexity with reference to mixing or coating processes. It is deemed to give constant or approximately steady weight ratio of alginate to covalently attached co-excipient in copolymers, thereby leading to controllable matrix processing and drug release. This review describes various grafting approaches and their outcome on oral drug release behaviour of alginate graft copolymeric matrices. It examines drug release modulation mechanism of alginate graft copolymers against that of co-excipients in non-grafted formulations. Key findings Drug release from alginate matrices can be modulated through using either co-excipients or graft copolymers via changing their swelling, erosion, hydrophobicity/ hydrophilicity, porosity and/or drug adsorption capacity. However, it is not known if the drug delivery performance of formulations prepared using alginate graft copolymers is superior to those incorporating graft-equivalent co-excipient physically in a dosage form without grafting but at the corresponding graft weight, owing to limited studies being available. Conclusions The value of alginate graft copolymers as the potential alternative to alginate-co-excipient physical mixture in oral drug delivery cannot be entirely defined by past and present research. Such an issue is complicated by the lack of green chemistry graft copolymer synthesis approach, high grafting process cost, complications and hazards, and the formed graft copolymers having unknown toxicity. Future research will need to address these matters to achieve a widespread commercialization and industrial application of alginate graft copolymers in oral drug delivery

show abstract

Design of In Situ Dispersible and Calcium Cross-Linked Alginate Pellets as Intestinal-Specific Drug Carrier by Melt Pelletization Technique

Cited by 19 publications

References 25 publications

Alginate–C18 Conjugate Nanoparticles Loaded in Tripolyphosphate-Cross-Linked Chitosan–Oleic Acid Conjugate-Coated Calcium Alginate Beads as Oral Insulin Carrier

Alginate–C18 Conjugate Nanoparticles Loaded in Tripolyphosphate-Cross-Linked Chitosan–Oleic Acid Conjugate-Coated Calcium Alginate Beads as Oral Insulin Carrier

Oral Fast-Release Solid Dispersion-Paradigm Shift to Nanoparticles

Alginate graft copolymers and alginate–co-excipient physical mixture in oral drug delivery

Contact Info

Product

Resources

About