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"Designed to support the development of new, effective therapeutics, Topical and transdermal drug delivery : principles and practice explains the principles underlying the field and then demonstrates how these principles are put into practice in the design and development of new drug products. Drawing together and reviewing the latest research findings, the book focuses on practical, tested, and proven approaches that are backed by industry case studies and the authors' firsthand experience. Moreover, the book emphasizes the mechanistic information that is essential for successful drug product development."

""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."

"Pengiriman obat melalui transdermal telah menjadi metode yang menjanjikan dalam mengatasi keterbatasan pengiriman obat secara konvensional. Teknologi inovatif seperti microneedle (MN) menawarkan solusi untuk menghindari degradasi obat dalam saluran pencernaan, mengatasi efek first pass terkait dengan hati, serta mengurangi rasa sakit dan ketidaknyamanan yang terkait dengan injeksi intravena. Salah satu jenis MN yang potensial adalah Hydrogel-Forming Microneedle (HFMN). Penelitian ini bertujuan untuk mengembangkan sediaan Hydrogel Forming Microneedle (HFMN) dari poli(vinil alkohol)/poli(N-vinil kaprolaktam) untuk pengiriman obat kaptopril secara transdermal. Sediaan HFMN dioptimalkan dengan variasi waktu crosslinking, konsentrasi PNVCL, dan konsentrasi asam sitrat. Evaluasi dilakukan melalui uji fisik, kekuatan mekanik, dan uji insersi. Kemampuan HFMN dalam menghantarkan obat diuji melalui uji permeasi in vitro menggunakan alat sel difusi Franz, dan penentuan kadarnya diukur menggunakan metode KCKT. Hasil penelitian menunjukkan bahwa waktu crosslinking dan konsentrrasi asam sitrat yang tepat dapat meningkatkan kekuatan mekanik HFMN serta penambahan PNVCL meningkatkan penetrasi, swelling, Permeabilitas dan kekuatan mekanik.. Formula HFMN yang paling optimal dalam meningkatkan permeasi obat kaptopril secara transdermal adalah F3 dengan nilai permeasi 66,68 ± 2,78 %, yang menunjukkan kinerja terbaik dalam memfasilitasi penetrasi obat kaptopril. Dengan demikian, sediaan HFMN ini menawarkan potensi sebagai metode pengiriman obat kaptopril secara transdermal yang efektif.

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Transdermal drug delivery has become a promising method in overcoming the limitations of conventional drug delivery. Innovative technologies such as microneedle (MN) offer solutions to avoid drug degradation in the gastrointestinal tract, overcome first pass effects associated with the liver, and reduce pain and discomfort associated with intravenous injection. One potential type of MN is Hydrogel-Forming Microneedle (HFMN). This study aimed to develop a Hydrogel Forming Microneedle (HFMN) preparation of poly(vinyl alcohol)/poly(N-vinyl caprolactam) for transdermal delivery of captopril drug. The HFMN preparation was optimised by varying crosslinking time, PNVCL concentration, and citric acid concentration. Evaluation was conducted through physical tests, mechanical strength, and insertion tests. The ability of HFMN to deliver drugs was tested through in vitro permeation test using Franz diffusion cell apparatus, and the determination of their levels was measured using the KCKT method. The results showed that appropriate crosslinking time and citric acid concentration could increase the mechanical strength of HFMN and the addition of PNVCL increased penetration, swelling, permeability and mechanical strength. The most optimal HFMN formula in increasing captopril drug permeation transdermally is F3 with a permeation value of 66.68 ± 2.78%, which shows the best performance in facilitating captopril drug penetration. Thus, this HFMN preparation offers potential as an effective transdermal drug delivery method of captopril."

"This book describes the theories, applications, and challenges for different oral controlled release formulations. This book differs from most in its focus on oral controlled release formulation design and process development. It also covers the related areas like preformulation, biopharmaceutics, in vitro-in vivo correlations (IVIVC), quality by design (QbD), and regulatory issues"

"Karvedilol adalah obat anti hipertensi golongan β-blocker yang biasa diresepkan sebagai terapi pengobatan jangka panjang hipertensi. Biaovaibilitas oral karvedilol terbilang rendah dan t ½ yang pendek menyebabkan frekuensi penggunaan obat yang lebih sering atau dosis penggunaan harus ditingkatkan. Rute transdermal menjadi solusi alternatif yang diperlukan untuk mengatasi hal tersebut. Patch transdermal adalah salah satu sistem pembawa transdermal yang dapat menghantarkan obat secara terkendali melalui kulit dalam periode waktu tertentu. Penelitian ini bertujuan memperoleh formula sesuai dengan karakter fisik patch transdermal, memperoleh data kinetika pelepasan obat serta data penetrasi patch transdermal karvedilol dengan sistem matriks. Ratio Polimer Polivinyl Alkohol (PVA) dan etil selulosa (ES) serta konsentrasi peningkat penetrasi Span 20 yang digunakan yaitu F1 (1:1 /8%),F2 (1:1 /10%), F3(2:1 /8%), F4(2:1 /10%). Formula F1 tidak lolos dalam evaluasi organoleptis sehingga uji selanjutnya hanya dilakukan pada formula F2, F3 dan F4. Pelepasan karvedilol secara in vitro menunjukkan formula F2, F3 dan F4 berlangsung selama 24 jam dan kinetika pelepasannya mengikuti orde 0 dan Higuchi. Uji penetrasi in vitro karvedilol menunjukkan % kumulatif karvedilol untuk formula F2, F3 dan F4 yaitu 15,384%, 16,495% dan 18,287%.

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Carvedilol is antihypertensive drug class of β-blockers commonly prescribed for long-term treatment of hypertension. Low oral bioavaibility and short 1/2 time of Carvedilol causes frequency of drug use more often or dose should be increased. Transdermal route become alternative solution overcoming it. Transdermal patch is a transdermal carrier system which deliver drug through skin in controlled within specific time period. This study aims to obtain formula with physical characteristic of transdermal patch, obtaining data of drug kinetic release and penetration of carvedilol in transdermal patch with matrix system. Ratio Polymer polyvinyl alcohol (PVA) and ethyl cellulose (EC) also penetration enhancers concentration of Span 20 used in the manufacture of transdermal patch were F1 (1:1 /8%), F2 (1:1 / 10%), F3 (2:1 /8%), F4 (2:1 /10%). Formula F1 was unqualified for organoleptic evaluation so the next evaluation only carried out for formulas F2, F3 and F4. The in vitro release of carvedilol studies showed formula F2, F3 and F4 lasted for 24 hours and release kinetics of drug followed orde 0 and Higuchi. The in vitro penetration test showed % cumulative carvedilol for the formula F2, F3 and F4 respectively were 15,384%,16,495% and 18,287%"

"Ketoprofen merupakan golongan AINS non selektif COX-2 yang umum digunakan sebagai pengobatan rheumatoid arthritis. Ketoprofen umumnya digunakan dalam bentuk sediaan oral, tetapi pemberian secara oral dapat menyebabkan ketoprofen mengalami first pass metabolism. Oleh karena itu, pemberian obat diubah melalui rute transdermal mikroemulsi agar dapat meningkatkan kelarutan ketoprofen pada penelitian ini. Namun, penetrasi ketoprofen obat secara transdermal tidak efisien, sehingga diperlukan penambahan kamfer sebagai peningkat penetrasi. Peneltian ini betujuan untuk memperoleh formulasi dengan stabilitas fisik yang optimum setelah diberikan penambahan kamfer dan melihat pengaruh kamfer pada berbagai konsentrasi terhadap penetrasi transdermal ketoprofen dalam sediaan mikroemulsi. Sediaan mikroemulsi dihasilkan dengan konsentrasi smix 45% dengan rasio smix 5:4 (25% tween 80: 20% propilen glikol), Virgin Coconut Oil 3%, etanol 3%, metil paraben 0,3%, propil paraben 0,05%, BHT 0,1%, dan konsentrasi kamfer 0% pada FA8, 1% pada FB8, 3% pada FC8, dan 5% pada FD8. Evaluasi keempat formulasi mikroemulsi dilakukan dengan pengukuran globul sediaan, tegangan permukaan, pH, viskositas, bobot jenis, pengamatan uji stabilitas fisik, cycling test, dan uji sentrifugasi. Uji penetrasi ketoprofen menunjukkan bahwa persentase jumlah kumulatif ketoprofen yang terpenetrasi pada FA8, FB8, FC8, dan FD8 secara berturut-turut sebesar 12,17%, 36,75%, 31,94%, 21,46%. Berdasarkan hasil penelitian disimpulkan bahwa keempat mikroemulsi yang dihasilkan jernih dan stabil selama pengamatan. Pada hasil uji penetrasi obat kumulatif, tingkat penetrasi pada FB8 yang mengandung kamfer sebesar 1% memberikan jumlah penetrasi zat aktif yang paling tinggi......Ketoprofen is a COX-2 non-selective NSAID which is commonly used as a treatment for rheumatoid arthritis. Ketoprofen is generally used in oral dosage forms, but oral administration can cause ketoprofen to undergo first pass metabolism. Therefore, the administration was changed to transdermal microemulsion dosage form to increase the solubility of ketoprofen in this study. However, transdermal penetration of ketoprofen is not efficient, so the addition of camphor is needed as a penetration enhancer. This study aims to obtain a formulation with optimal physical stability after the addition of camphor and to see the effect of camphor at various concentrations on transdermal penetration of ketoprofen in microemulsion preparations. Microemulsion preparation was produced from 45% smix concentration with a 5:4 smix ratio (25% tween 80: 20% propylene glycol), 3% Virgin Coconut Oil, 3% ethanol, 0,3% methyl paraben, 0,05% propyl paraben, 0,1% BHT, and the concentration of 0% camphor on FA8, 1% on FB8, 3% on FC8, and 5% on FD8. The evaluation of four ketoprofen microemulsion formulations with the following smix ratio and camphor concentrations was carried out by examinating size of globule, surface tension, pH, viscosity, specific gravity, physical stability, cycling, and centrifugation. Ketoprofen penetration test showed the cumulative penetration of the FA8, FB8, FC8, and FD8 formulation were 12,17%, 36,75%, 31,94%, and 21,46%, respectively. To conclude, the four microemulsion preparations were clear and stable. Cumulative drug penetration test showed the penetration rate of FB8 with 1% camphor gave the highest penetration result."

"Patch transdermal (transdermal patch) adalah plester berperekat khusus yang mengandung obat, yang dirancang untuk ditempelkan pada kulit. Tujuannya adalah untuk memberikan dosis obat yang tepat melalui kulit dan masuk ke dalam aliran darah. Dalam penelitian ini, patch transdermal yang berbasis polimer alami diformulasikan menggunakan campuran pati sagu (Metroxylon sagu) dan HPMC (Hidroksipropil Metilselulosa) dengan teknik solvent casting. Penelitian ini bertujuan untuk memformulasi dan mengevaluasi patch transdermal dari polimer pati sagu. Carvedilol digunakan sebagai obat yang diantarkan melalui patch transdermal berbasis pati sagu/HPMC. Penambahan Polietilen Glikol dilakukan sebagai plastisizer untuk meningkatkan sifat fisikokimia polimer. Patch transdermal yang dihasilkan menunjukkan permukaan yang homogen berdasarkan citra SEM dengan massa yang konsisten berkisar 20,9 - 21,07 mg/cm2 dan ketebalan 0,22 - 0,24 mm. Formulasi dengan komposisi pati sagu yang tinggi juga menunjukkan kadar kelembapan yang lebih rendah (< 4%). Uji pelepasan Carvedilol secara in-vitro menunjukkan percepatan pelepasan obat pada formulasi dengan komposisi HPMC yang tinggi yaitu hingga 62,47%. Hasil penelitian ini berhasil menunjukkan karakteristik polimer pati sagu/HPMC dengan penambahan Polietilen Glikol sebagai plastisizer pada aplikasi patch transdermal.

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A transdermal patch is a special adhesive plaster containing medication, which is designed to be attached to the skin. The goal is to deliver the correct dose of medication through the skin and into the bloodstream. In this research, a natural polymer-based transdermal patch was formulated using a mixture of sago starch (Metroxylon sago) and HPMC (Hydroxypropyl Methylcellulose) using the solvent casting technique. This study aims to formulate and evaluate a transdermal patch from sago starch polymer. Carvedilol is used as a drug delivered via a sago starch/HPMC based transdermal patch. The addition of Polyethylene Glycol is carried out as a plasticizer to improve the physicochemical properties of the polymer. The resulting transdermal patch showed a homogeneous surface based on SEM images with a consistent mass ranging from 20.9 - 21.07 mg/cm2 and a thickness of 0.22 - 0.24 mm. Formulations with a high sago starch composition also show lower moisture content (< 4%). The in-vitro Carvedilol release test showed accelerated drug release in formulations with a high HPMC composition, namely up to 62.47%. The results of this research succeeded in showing the characteristics of sago starch/HPMC polymer with the addition of Polyethylene Glycol as a plasticizer in transdermal patch applications."

"Telah dikembangkan formulasi sediaan transdermal gel glukosamin yang menggunakan senyawa enhancer: etanol,  propilen glikol,  dan  gliserin. Kemampuan penetrasi perkutan formulasi sediaan tersebut dievaluasi dengan uji penetrasi perkutan in vitro menggunakan sel difusi Franz melalui penambahan 1 g sediaan gel glukosamin 1% ke dalam kompartemen donor dan uji ketersediaan hayati in vivo pendahuluan menggunakan seorang subyek manusia sehat melalui aplikasi selama 10 jam dosis tunggal 10 g sediaan gel glukosamin 1% di kedua lututnya. Jumlah kumulatif glukosamin yang terpenetrasi dari formula kontrol, formula I (etanol 3%), formula II (etanol 5%), formula III (propilen glikol 1%), formula IV (propilen glikol 3%), formula V (gliserin 1%), dan formula VI (gliserin 3%) setelah 180 menit secara berturut-turut adalah sebanyak 76,4836 ± 2,3479; 417,8439 ± 18,9042; 583,1494 ± 5,9162; 152,1894 ± 1,5184; 515,1065 ± 14,0069; 83,0822 ± 0,0364; dan 478,6089 ± 3,7406 µg.cm^-². Laju penetrasi atau fluks rata-rata glukosamin dari formula kontrol, formula I, formula II, formula III, formula IV, formula V, dan formula VI selama 180 menit secara berturut-turut adalah 24,4453; 123,608; 167,5478; 47,0377; 164,603; 28,7548; dan 139,3895 µg.cm^-2.jam^-1. Waktu laten dari formula kontrol, formula I, formula II, formula III, formula IV, formula V, dan formula VI secara berturut-turut adalah 13,89; 10,24; 9,75; 13,05; 10,04; 13,51 menit, dan tidak dapat diekstrapolasikan. Profil ketersediaan hayati menunjukkan C_maks, t_maks, dan AUC_0-10 dari formula II dan formula kontrol secara berturut-turut adalah 310,56 ng.mL^-1, jam ke-5, dan 2079,85 ng.mL^-1.jam; 285,79 ng.mL^-1, jam ke-5, dan 1921,65 ng.mL^-1.jam.

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A transdermal formulation of glucosamine gel using skin penetration enhancers, i.e. ethanol, propylene glycol, and glycerin had been developed. Penetration ability of the formulation was evaluated by in vitro penetration study using Franz diffusion cell with 1 g glucosamine gel 1% applied into the donor compartment and in vivo preliminary bioavailability study of a healthy male subject received a single dose of 10 g glucosamine gel 1% on both knees as long as 10-hour applications. Cumulative amount of glucosamine penetrated from control, formula I (ethanol 3%), formula II (ethanol 5%), formula III (propylene glycol 1%), formula IV (propylene glycol 3%), formula V (glycerin 1%), and formula VI (glycerin 3%) after 180 minutes penetration study were 76.4836 ± 2.3479; 417.8439 ± 18.9042; 583.1494 ± 5.9162; 152.1894 ± 1.5184; 515.1065 ± 14.0069; 83.0822 ± 0.0364; and 478.6089 ± 3.7406 µg.cm^-² respectively. Mean flux of glucosamine from control, formula I, formula II, formula III, formula IV, formula V, and formula VI within 180 minutes were 24.4453; 123.608; 167.5478; 47.0377; 164.603; 28.7548; and 139.3895 µg.cm^-2.hour^-1 respectively. Lag time for steady-state of control, formula I, formula II, formula III, formula IV, formula V, and formula VI were 13.89; 10.24; 9.75; 13.05; 10.04; 13.51 minutes, and unextrapolated one, respectively. The bioavailability profile showed the C_max, t_max, and AUC_0-10 of formula II and control were 310.56 ng.mL^-1, 5 hours, and 2079.85 ng.mL^-1.hour; 285.79 ng.mL^-1, 5 hours, and 1921.65 ng.mL^-1.hour respectively."