Chitosan Nanoparticles as a Novel Drug Delivery System: A Review Article

Natural polymers, particularly polysaccharide, have been used as drug delivery systems for a variety of therapeutic agents such as peptides, proteins, vaccines, DNA, and drugs for parenteral and non-parenteral administration. Chitosan, the second most abundant naturally occurring polysaccharide after cellulose, is a biocompatible and biodegradable mucoadhesive polymer that is extensively used in the preparation of nanoparticles (NPs). Chitosan NPs loaded with drugs were found to be stable, permeable and bioactive. In this review, the importance of chitosan and its derivatives in drug delivery is illustrated, different methods of preparation of chitosan and chitosan derivatives NPs and their physio- chemical properties are addressed. Moreover, the desirable characteristics of successful NPs based drug delivery systems, as well as the pharmaceutical applications of these NPs are also clearly explored.

Pengaruh Polivinilpirolidon sebagai Polimer Mukoadhesif terhadap Sifat Fisik Patch Ekstrak Kulit Buah Delima (Punica granatum L.)

ABSTRAKBuah delima (Punica granatum L.) secara empiris digunakan untuk mengobati masalah gigi dan mulut seperti sariawan. Pengembangan obat sariawan berbasis herbal dengan bentuk sediaan patch dilakukan untuk mempertahankan waktu kontak antara zat aktif dengan bagian sariawan. Polivinilpirolidon (PVP) digunakan sebagai polimer karena sifatnya mukoadhesif sehingga mampu berikatan pada mukosa mulut. Penelitian ini bertujuan untuk mengetahui pengaruh penggunaan PVP sebagai polimer mukoadhesif terhadap karakteristik fisik sediaan patch yang mengandung ekstrak kulit buah delima (EKBD). EKBD diperoleh dengan metode maserasi. Konsentrasi EKBD yang digunakan adalah 5% dan 10%. Sedangkan konsentrasi polimer PVP yang digunakan yaitu 30,29%, 33,04, 48,75%, dan 65,5%. Patch selanjutnya akan di evaluasi fisik yang meliputi keseragaman bobot dan dimensi ketebalan, pH permukaan, swelling, daya lekat, dan waktu lekat. Hasil menunjukkan bahwa patch yang mengandung ekstrak 10% dengan tambahan polimer konsentrasi 30,29% memiliki sifat yang cukup elastis disbanding dengan konsentrasi 48,75% dan 65,5%. Sedangkan uji evaluasi fisik menghasilkan keseragaman bobot dan dimensi yang seragam, pH 6,63, rata-rata indeks swelling 40,69% ± 16, dan rata-rata daya dan waktu lekat 13,50 ± 11,6. Dengan demikian dapat disimpulkan bahwa konsentrasi PVP terbukti berpengaruh pada sifat fisik patch yang dihasilkan. Kata kunci : Polivinilpirolidon; Ekstrak Kulit Buah Delima; Patch.ABSTRACTPomegranate (Punica granatum L.) is empirically used to treat dental and mouth problems such as reccurent aphthous stomatitis (RAS). The development of RAS therapy based on herbal with patches dosage forms is carried out to maintain the contact time between the active substance and the RAS. Polyvinylpyrrolidone (PVP) is used as a polymer because it is mucoadhesive, so it can bind to the oral mucosa. Aimed to determine the effect of the use of PVP as a mucoadhesive polymer on the physical characteristics of patches preparations containing pomegranate peel extract (PPE). PPE was obtained by maceration method. The PPE concentration used were 5% and 10%. PVP concentration used were 30.29%, 33.04%, 48.75%, and 65.5%. The patches properties such as uniformity of thickness, pH, swelling index, tensile and mucoadhesive strength. The results showed that patches containing 10% extract and PVP concentration of 30.29% had sufficient elastic properties compared to both concentration. While the physical evaluation test obtained uniform weights and dimensions that are uniform, pH 6.63, the average swelling index is 40.69% ± 16, and the tensile and mucoadhesive strength is 13.50 ± 11.6. Altogether, the concentration of PVP is proven to affect the physical properties of the resulting patch.Key word : Polyvinylpyrrolidone; Pomegranate Peel Extract; Patch.

Mucoadhesive Pellets for Drug Delivery Applications: A Critical Review

Pellets are spherical shaped multiparticulate drug delivery systems with size ranging between 0.5-2.0 mm. Free flow, good mechanical properties, improved physical and chemical properties of powder, and stability are some advantages of pellets. Mucoadhesive pellets could be developed by using appropriate concentration and type of mucoadhesive polymer. Mucoadhesive pellets can be used for delivery of drugs to gastric, colonic, and vaginal regions. Immediate release, sustained/controlled release and implantable delivery could be incorporated using mucoadhesive pellets. Reproducibility, ease of scalability, quality control checks and significant mechanical strength are some advantages making pellets widely acceptable by pharmaceutical industry. In the present review, mucoadhesion process and theories, mucoadhesive polymers, pelletization process, evaluation of pellets and reported research/patents on mucoadhesive pellets for delivery of different categories of drugs have been presented.

Preparation iiand characterization of mucoadhesive microcapsules of paclitaxel

The objective of the present work was to develop paclitaxel encapsulated mucoadhesive microcapsules with an aim to enhance its efficacy and control the drug release in cancer patients. Paclitaxel microcapsules with a coat consisting of sodium alginate and mucoadhesive polymer such as acacia, Carbomer 941, Povidone K-30, Macrogol (PEG 6000) were prepared by ionotropic gelation technique and were evaluated for morphological characters, drug content, loading efficiency, drug–polymer interactions, swelling ratio, mucoadhesive properties and in vitro drug release. The resulting microcapsules were discrete, spherical, and free-flowing with a particle size range of 534 to 822 µm. The microencapsulation efficiency was 45.09–99.83%. The microcapsules prepared with alginate along with macrogol (F4M) have exhibited good mucoadhesive property in the in vitro wash off test. The swelling ratio of microcapsules was enhanced with increased alginate concentration and the formulation (F4) showed highest swelling index of 2666. Paclitaxel release from these mucoadhesive microcapsules was slow and extended over a period of 6 h and further depends upon the concentration of the alginate. The percent drug release of alginate-acacia microcapsules (F4Ac) was higher than other formulations in the present study. In conclusion, alginate-acacia mucoadhesive microcapsules could be promising vehicle for oral controlled release of paclitaxel.

Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A

The physiological protective mechanisms of the eye reduce the bioavailability of topically administered drugs above all for those with high molecular weight and /or lipophilic characteristics, such as Cyclosporine A (CyA). The combined strategy based on the association of nanomicelles and mucoadhesive polymer seems promising since a limited number of commercial products containing CyA have been recently approved. The scope of this investigation was the design of Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano), based on a binary system of two surfactants in combination with hyaluronic acid, and their biopharmaceutical evaluation. The optimisation of the ASMP-Nano in term of the amount of surfactants, CyA-loading and size determined the selection of the clear and stable Nano1HAB-CyA formulation containing 0.105% w/w CyA loaded-nanomicelles with a size of 14.41 nm. The nanostructured system had a protective effect towards epithelial corneal cells with a cell viability of more than 80%. It interacted with cellular barriers favouring the uptake and the accumulation of CyA into the cells as evidenced by fluorescent probe distribution, by hindering CyA permeation through reconstituted corneal epithelial tissue. In pharmacokinetics study on rabbits, the nanomicellar carrier prolonged the CyA retention time in the precorneal area mainly in presence of hyaluronic acid (HA), a mucoadhesive polymer.