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"Written for busy professionals at the forefront of new drug development, "Drug delivery" gets readers quickly up to speed on both the principles and latest applications in the increasingly important field of drug delivery. Recent developments in such areas as combinatorial chemistry, proteomics, and genomics have revolutionized researchers' ability to rapidly identify and synthesize new pharmacological compounds. However, delivery-related properties remain a significant reason for clinical trial failures. It begins with an in-depth review of key fundamentals, such as physiochemical and biological barriers; drug delivery pathways; metabolism; drug formulation; pharmacokinetic and pharmacodynamic issues; and more. The remainder of the book is devoted to the systematic examination, including overviews, timely examples, and extensive references, of a host of specific subjects."

"Nanoemulsi donepezil yang dihantarkan dari hidung ke otak dapat menjadi alternatif untuk meningkatkan akumulasi donepezil di otak dan menghindari efek samping di saluran cerna. Namun, penelitian sebelumnya masih menggunakan konsentrasi surfaktan yang dapat menimbulkan sitotoksisitas. Penelitian ini bertujuan untuk menghasilkan nanoemulsi donepezil dengan droplet berukuran di bawah 200 nm, nilai potensial zeta lebih besar dari 30 mV, indeks polidispersitas kurang dari 0,3, pH mendekati pH fisiologis nasal, serta fluks permeasi in vitro yang lebih tinggi dari kontrol. Nanoemulsi m/a yang mengandung donepezil, asam oleat, Tween 80, PEG 400, BHT, dan air demineralisata dibentuk dengan metode homogenisasi kecepatan tinggi dan ultrasonikasi. Parameter organoleptis, ukuran, indeks polidispersitas, potensial zeta, pH, permeasi in vitro melalui mukosa nasal kambing, dan stabilitas tiga formula nanoemulsi yang mengandung 3%, 4%, dan 5% surfaktan dinilai dan dibandingkan. Ketiga nanoemulsi memiliki ukuran droplet di bawah 110 nm, potensial zeta mencapai -29,77 mV, indeks polidispersitas kurang dari 0,3, pH masih ditoleransi mukosa nasal, dan stabil dalam penyimpanan pada suhu 30 ± 2 °C maupun 5 ± 2 °C selama sebulan. Melalui studi ini disimpulkan bahwa nanoemulsi F2 memiliki karakteristik fisik yang baik dan fluks permeasi terbaik (9,51 ± 2,64¼g/cm2.jam) sehingga berpotensi digunakan untuk meningkatkan akumulasi donepezil di otak.

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Donepezil nanoemulsion delivered via the nose to brain route can be an alternative to increase donepezil accumulation in the brain and avoid gastrointestinal side effects. However, previous study still used high surfactant concentrations which can cause cytotoxicity. This study aims to produce donepezil nanoemulsions with droplet sizes below 200 nm, zeta potential values greater than 30 mV, polydispersity index less than 0.3, pH nearing nasal physiological pH, and higher in vitro permeation compared to control. An o/w nanoemulsion comprising of donepezil base, oleic acid, Tween 80, PEG 400, BHT, and demineralized water was formed by high-speed homogenization and ultrasonication. Organoleptic, size, polydispersity index, zeta potential, pH, in vitro permeation through goat nasal mucosa, and the stability of three formulas containing 3%, 4%, and 5% surfactant were compared. All three nanoemulsions had droplet sizes below 110 nm, zeta potential up to -29.77 mV, polydispersity index less than 0.3, pH tolerated by nasal mucosa, and stable in storage at 30 ± 2 °C and 5 ± 2 °C for a month. This study concludes that the F2 nanoemulsion had good physical characteristics and the best permeation flux (9,51 ± 2,64¼g/cm2.hour), thus having potential to increase donepezil accumulation in the brain."

""By understanding the mechanisms by which compounds cross the skin, it becomes possible to devise means for improving drug delivery. Providing an overview of the current science in drug and cosmetic application to and through the skin, Topical and Transdermal Drug Delivery includes treatment of skin conditions, skin permeation, and enhancement and measurement of skin permeation. The book provides pharmaceutical scientists, skin product development experts, and those in the cosmetic and personal care industry with practical knowledge and insight into future product development"--Provided by publisher."

"Pirfenidon yang dihantarkan secara peroral mengalami metabolisme lintas pertama, sehingga memerlukan dosis tinggi dan berpotensi menyebabkan efek samping sistemik. Oleh karena itu, pengembangan rute alternatif bagi pirfenidon perlu dilakukan. Penelitian sebelumnya melaporkan bahwa sistem penghantaran intrapulmonal berbasis solid lipid nanoparticles (SLN) dapat terdeposit dengan baik pada area alveolus paru-paru. Namun, karakteristik SLN dapat dipengaruhi oleh rasio lipid terhadap obat, jenis dan konsentrasi polimer. Oleh karena itu, optimisasi dengan metode permukaan respon perlu dilakukan untuk memperoleh formula SLN pirfenidon (P-SLN) yang optimal untuk penghantaran intrapulmonal. Lima belas formula disusun berdasarkan desain Box Behnken dengan tiga faktor yaitu, rasio lipid terhadap obat, jenis polimer dan konsentrasi polimer, serta tiga respon, meliputi ukuran partikel, PDI dan efisiensi penjerapan. Formula P-SLN optimal dikarakterisasi meliputi morfologi, kadar lembab, performa aerodinamik, studi disolusi dan stabilitas. Hasil optimisasi menunjukkan bahwa P-SLN optimal tersusun dari rasio lipid terhadap obat 6:1 dan 0,5% Plasdone K-29/32 (FO1). P-SLN FO1 memiliki bentuk sferis dengan ukuran partikel 212,67 nm, PDI 0,39, efisiensi penjerapan 95,02%, dan kadar lembab 1,59%. FO1 memiliki mass median aerodynamic diameter berkisar antara 0,54–12,12 μm. Selain itu, FO1 melepaskan pirfenidon sebanyak 89,61% dan 69,28% dalam medium pH 4,5 dan pH 7,4 selama 45 menit. Sebagai kesimpulan, FO1 terbukti memiliki karakteristik yang sesuai untuk menghantarkan pirfenidon melalui rute intrapulmonal.

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Orally administration of pirfenidone undergoes first-pass metabolism, hence requires high dose level and leads to systemic side effects. Therefore, it is necessary to develop an alternative route of administration for pirfenidone. Previous research reported that the solid lipid nanoparticle-based (SLN) intrapulmonary drug delivery system (IPDDS) was deposit well in the alveolar region of the lungs. However, the characteristics of SLN could be influenced by lipid-to-drug ratio, polymer type and concentration. Therefore, optimization using response surface methodology was carried out to obtain the optimized pirfenidon-loaded SLN (P-SLN) formula for IPDDS. Box-Behnken design was applied to create 15 formulas comprising three factors, including lipid-to-drug ratio, type and concentration of polymer and three responses, including particle size, PDI and entrapment efficiency. The optimized P-SLN formula was characterized, including morphology, moisture content, aerodynamic performance, dissolution and stability studies. The optimization results yielded an optimized P-SLN comprised a lipid-to-drug ratio of 6:1 and 0.5% Plasdone K-29/32 (FO1). The P-SLN FO1 had a spherical shape with a particle size of 212.67 nm, PDI of 0.39, entrapment efficiency of 95.02%, and moisture content of 1.59%. FO1 had a mass median aerodynamic diameter ranging from 0.54–12.12 μm. In addition, FO1 release 89.61% and 69.28% pirfenidone for 45 minutes in buffer medium pH 4.5 and pH 7.4. In conclusion, FO1 was proven to have an appropriate IPDDS characteristics for delivering pirfenidone."

"Alginat adalah salah satu polisakarida alami yang dapat ditemukan pada sejumlah aplikasi biomedis. Hal ini didukung oleh sifatnya, yaitu biokompatibel, rendah kadar toksisitas, kelimpahan ketersediaannya, dan kemudahan proses gelasinya. Untuk meningkatkan sifat biodegradasi dan kemampuan interaksinya dengan sel tubuh, maka diperlukan modifikasi lanjut untuk senyawa alginat. Pada penelitian ini ditelaah metoda konjugasi alginat dengan reaksi oksidasi periodat dan reduksi aminasi. Penelitian diawali dengan pemetaan potensi protein dari sejumlah koleksi alga Indonesia. Kemudian dilanjutkan dengan konjugasi alginat dengan benzilamina dan ?-lisin. Kondisi reaksi optimal konjugasi dipelajari dengan menelaah pengaruh rasio substrat dengan oksidator dan reduktor. Alginat yang dikonjugasikan dengan benzilamina, mampu bertindak sebagai surfaktan karena membentuk misel pada pH asam, sedangkan dari senyawa alginat terkonjugasi ?-lisin, diperoleh produk berupa hidrogel dengan metoda pembentukan ikatan silang basa Schiff menggunakan gelatin. Hidrogel ini memiliki keunggulan karena ikatan yang terbentuk berupa pseudokovalen, menghasilkan hidrogel sifat self-healing. Dengan menggunakan kondisi konjugasi optimal, maka metoda modifikasi selanjutnya digunakan untuk membentuk alginat terkonjugasi lektin wheat germ aggulitinin (WGA). Mikropartikel dari alginat terkonjugasi WGA disintesis dengan metoda emulsifikasi dan ikatan silang ionik. Mikropartikel kemudian dimuat dengan kurkumin, pola pelepasan, hemakompatabilitas dan sitotoksisitinya diamati. Hasil penelitian menunjukkan enkapsulasi kurkumin dengan mikropartikel menghasilkan model pelepasan yang diperpanjang, dan pada konsentrasi rendah mikropartikel menunjukkan sifat hemakompatibel.

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Alginates are one of the natural polysaccharides that are found in numerous applications in biomedical science and engineering. This is due to the favorable properties of alginates, including biocompatibility, low toxicity, abundant availability, and ease of gelation. Chemical functionalization is one way to generate alginate derivatives with low molecular weight and high cell interactions. In this research conjugation method via periodate oxidation and reductive amination was studied. The research began with algae protein’s potential mapping from a few of Indonesian algae collection. The second part of the research was to conjugate the alginate with benzylamine and ?-lysine. We studied the effect of substrates against oxidation and reduction agents towards reaction yields. The benzylamine conjugated alginate was producing micelle on acidic pH, makes it suitable to acts as surfactant. From the ?-lysine conjugated alginate, we produced hydrogel by using gelatin to form Schiff base crosslinking. This hydrogel was linked by pseudocovalent linker which generates its self-healing properties. With conjugation optimum condition, alginate was conjugated with WGA lectin. Microparticles from alginate conjugated WGA were prepared through emulsification and ionic crosslinking. The microparticle was loaded with curcumin. The released pattern, hemacompatability and cytotoxicity of microparticle were investigated. The results show that encapsulation of curcumin with microparticle was released in prolonged manner and at low concentration, microparticle was hemocompatible."

"Current pharmaceutical and clinical approaches to the treatment of disease suffer from the inherent limitations in the specialization of drugs introduced to physiological systems. The interface of clinical and material sciences has allowed for a broad spectrum of creative approaches with the potential to alleviate these shortcomings. However, the synergy of these disciplines also presents problems in which nascent technology lacks the necessary evaluation within its intended clinical environment. Given the growing potential for materials science to address a number of unanswered therapeutic needs, it remains even more pressing to validate emerging drug delivery technologies in actual clinical environments. This book addresses the core fundamentals of drug delivery using material science and engineering principles, and then applies this knowledge using prominent examples from both the scientific literature and clinical practice"

"Amoksisilin trihidrat memiliki waktu tinggal yang singkat di dalam lambung. Penghantaran obat dengan sistem mengapung dikembangkan agar sediaan dapat dipertahankan di lambung dalam waktu yang lama. Pada penelitian ini, disintesis hidrogel full-IPN kitosan-PNVP sebagai sediaan penghantar obat amoksisilin trihidrat dengan sistem mengapung yang mengandung agen pembentuk pori NaHCO3 dan CaCO3 dengan komposisi kitosan:PNVP 70:30 (% b/b), 2% asetaldehida 0,1 M, 1% inisiator amonium persulfat (APS), 1% MBA, waktu polimerisasi 0,5 jam, dan variasi konsentrasi 0%; 1%; 5%; 10%; dan 15% NaHCO3 dan CaCO3. Karakterisasi hidrogel dilakukan dengan menggunakan spektrofotometer FTIR, dan mikroskop stereo optik. Pengujian yang dilakukan diantaranya adalah uji porositas, uji daya apung in vitro, efisiensi penjerapan serta pelepasan amoksisilin trihidrat pada pH 1,2. Hidrogel full-IPN NaHCO3 menunjukkan porositas yang lebih besar dengan waktu awal mengapung yang lebih singkat daripada hidrogel full-IPN CaCO3 dan keduanya dapat membuat matriks mengapung lebih dari 12 jam. Hidrogel full-IPN CaCO3 menunjukkan pola pelepasan yang terkontrol dan efisiensi penjerapan amoksisilin yang lebih tinggi daripada NaHCO3. Konsentrasi agen pembentuk pori yang menghasilkan penjerapan dan pelepasan amoksisilin trihidrat yang optimum dari matriks hidrogel yaitu 5% NaHCO3 dan 10% CaCO3.

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Amoxicillin trihydrate has a short residence time in the stomach. Floating drug delivery systems were prepared to prolong the presence of the dosage form within the stomach at the desire period of time. In this research, full-IPN hydrogel chitosan-PNVP as carrier for floating drug delivery of amoxicillin trihydrate containing NaHCO3 and CaCO3 as pore forming agents were synthesized with the composition chitosan: PNVP 70:30 (% w/w), 2% acetaldehyde 0.1 M, 1% initiator ammonium persulfate (APS), 1% MBA, 0.5 hours of the polymerization reaction time, and variation of the concentration 0%; 1%; 5%; 10%; and 15% of NaHCO3 and CaCO3. The hydrogels and microcapsules were characterized by FTIR spectrophotometer and stereo microscope. The effect of pore forming agents on the porosity, in vitro bouyancy, drug entrapment efficiency, and in vitro release were investigated. Hydrogel which contained NaHCO3 showed higher porosity with shorter floating lag time than CaCO3 and both been able to make the hydrogels floating more than 12 hours. CaCO3 incorporated hydrogels showed controlled drug release profile and higher drug entrapment efficiency than NaHCO3. The concentration of pore forming agents which had an optimum drug entrapment efficiency and release were found at 5% NaHCO3 and 10% CaCO3 pore forming agents."