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Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration
Din, Fakhar ud,Choi, Ju Yeon,Kim, Dong Wuk,Mustapha, Omer,Kim, Dong Shik,Thapa, Raj Kumar,Ku, Sae Kwang,Youn, Yu Seok,Oh, Kyung Taek,Yong, Chul Soon,Kim, Jong Oh,Choi, Han-Gon Informa UK (TaylorFrancis) 2017 DRUG DELIVERY Vol. No.
( Yeung Keun Choi ),( Fakhar Ud Din ),( Dong Wuk Kim ),( Yong Ll Kim ),( Jong Oh Kim ),( Sae Kwang Ku ),( Jeong Chan Ra ),( Jae Wook Huh ),( Jangik L Lee ),( Dong Hwan Sohn ),( Chul Soon Yong ),( Han 영남대학교 약품개발연구소 2014 영남대학교 약품개발연구소 연구업적집 Vol.24 No.0
The conservative single-layered wound dressing system is decomposed when mixed in polyvinyl alcohol (PVA) solution, which means it cannot be used with a temperature-sensitive drug. The goal of this investigation was to make an amniotic membrane extract (AME)-loaded double-layered wound dressing with an improved healing result compared to the conservative single-layered wound dressing systems. The double-layered wound dressing was developed with PVA/sodium alginate using a freeze-melting technique; one layer was PVA layer and the other was the drug-loaded sodium alginate layer. Its gel properties were assessed compared to single-layered wound dressings. Moreover, in vivo wound-healing effects and histopathology were calculated compared to commercial products. The double-layered wound dressing gave a similar gel fraction and Young`s module as single-layered wound bandages developed with only PVA, and a similar inflammation ability and WVTR as single-layered wound dressings developed with PVA and sodium alginate. Our data indicate that these double-layered wound bandages were just as swellable, but more elastic and stronger than single-layered wound dressings comprised of the same polymers and quantities, possibly giving an acceptable level of moisture and accumulation of exudates in the wound zone. Compared to the commercial product, the double-layered wound dressing comprising 6.7% PVA, 0.5% sodium alginate and 0.01% AME significantly enhanced the wound-healing effect in the wound-healing test. Histological investigations showed that superior full-thickness wound-healing effects compared to the commercial product. Therefore, the double-layered wound dressing would be an outstanding wound-dressing system with improved wound healing and good gel property.
( Dong Hoon Oh ),( Fakhar Ud Din ),( Dong Wuk Kim ),( Jong Oh Kim ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2014 영남대학교 약품개발연구소 연구업적집 Vol.24 No.0
A unique flurbiprofen-loaded nanoemulsion was listed earlier using a Shirasu porous glass (SPG) membrane emulsification technique, which gave constant emulsion droplets with a thin size distribution. In this study, a flurbiprofen-loaded nanoemulsion was developed further into a solid form using polyvinylpyrrolidone (PVP) as a carrier by a spray-drying technique. The flurbiprofen-loaded nanoparticles with a weight ratio of flurbiprofen/PVP/surfactant mixture of 1/8/2 were connected with about 130,000-fold enhanced drug solubility and had a mean size of about 70nm. In these nanoparticles, flurbiprofen was found in an altered amorphous state. Additionally, the nanoparticles gave significantly shorter T(max), and greater AUC and C(max) compared to the commercially available product. Specially, the AUC of the drug from the nanoparticles was about 10-fold greater compared to the commercially available product. Therefore, these flurbiprofen-loaded nanoparticles can be convenient for distributing a poorly water-soluble flurbiprofen with improved bioavailability using uniform nano-sized particles.
Rashid, Rehmana,Kim, Dong Wuk,Yousaf, Abid Mehmood,Mustapha, Omer,Din, Fakhar ud,Park, Jong Hyuck,Yong, Chul Soon,Oh, Yu-Kyoung,Youn, Yu Seok,Kim, Jong Oh,Choi, Han-Gon Dove Medical Press 2015 INTERNATIONAL JOURNAL OF NANOMEDICINE Vol.10 No.-
<P><B>Background</B></P><P>The objective of this study was to compare the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezetimibe-loaded solid self-nanoemulsifying drug delivery system (SNEDDS), surface modified solid dispersion (SMSD), and solvent evaporated solid dispersion (SESD) to identify the best drug delivery system with the highest oral bioavailability.</P><P><B>Methods</B></P><P>For the liquid SNEDDS formulation, Capryol 90, Cremophor EL, and Tween 80 were selected as the oil, surfactant, and cosurfactant, respectively. The nanoemulsion-forming region was sketched using a pseudoternary phase diagram on the basis of reduced emulsion size. The optimized liquid SNEDDS was converted to solid SNEDDS by spray drying with silicon dioxide. Furthermore, SMSDs were prepared using the spray drying technique with various amounts of hydroxypropylcellulose and Tween 80, optimized on the basis of their drug solubility. The SESD formulation was prepared with the same composition of optimized SMSD. The aqueous solubility, dissolution, physicochemical properties, and pharmacokinetics of all of the formulations were investigated and compared with the drug powder.</P><P><B>Results</B></P><P>The drug existed in the crystalline form in SMSD, but was changed into an amorphous form in SNEDDS and SESD, giving particle sizes of approximately 24, 6, and 11 µm, respectively. All of these formulations significantly improved the aqueous solubility and dissolution in the order of solid SNEDDS ≥ SESD > SMSD, and showed a total higher plasma concentration than did the drug powder. Moreover, SESD gave a higher area under the drug concentration time curve from zero to infinity than did SNEDDS and SMSD, even if they were not significantly different, suggesting more improved oral bioavailability.</P><P><B>Conclusion</B></P><P>Among the various formulations tested in this study, the SESD system would be strongly recommended as a drug delivery system for the oral administration of ezetimibe with poor water solubility.</P>
( Dong Wuk Kim ),( Yong Il Kim ),( Hong Hee Han ),( Fakhar Ud Din ),( Kwan Hyung Cho ),( Jong Oh Kim ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2014 영남대학교 약품개발연구소 연구업적집 Vol.24 No.0
To develop a novel triamcinolone acetonide (TAA)-loaded spray for the treatment of stomatitis, several spray solutions were prepared using various amounts of TAA, Eudragit L100 (Eudragit L) and PEG 400, and 100 ml ethanol. Their viscosity and spraying potential were investigated, with the result that the spraying threshold was 9.5 cP. The effect of PEG 400 on the properties of films formed after spraying was assessed. Its anti-inflammatory effect in mice was evaluated and compared to a commercial product. As the PEG 400 concentration increased, the film elongation and washability by the saliva solution increased, and tensile strength decreased. PEG 400 had little effect on mucoadhesive force and drug release. The TAA-loaded spray solution containing TAA, Eudragit L, PEG 400 and ethanol at the ratio of 1:6:3:100 (w/w/w/v) was easy to spray onto stomatitis lesions in the mouth via a spraying vessel incorporating a long straw. After spraying, the TAA-loaded spray formed a film with suitable elongation, tensile strength and washability that attached onto the mucosal membrane and released the drug. Moreover, it had excellent anti-inflammatory properties, similar to those of the commercial product. Thus, this novel TAA-loaded spray solution was easy to administer, had good film properties and excellent anti-inflammatory efficacy, and is therefore a potential candidate for the treatment of stomatitis.
( Dong Wuk Kim ),( Yong Il Kim ),( Hong Hee Han ),( Fakhar Ud Din ),( Kwan Hyung Cho ),( Jong Oh Kim ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2015 영남대학교 약품개발연구소 연구업적집 Vol.25 No.-
To develop a novel triamcinolone acetonide (TAA)-loaded spray for the treatment of stomatitis, several spray solutions were prepared using various amounts of TAA, Eudragit® L100 (Eudragit L) and PEG 400, and 100 ml ethanol. Their viscosity and spraying potential were investigated, with the result that the spraying threshold was 9.5 cP. The effect of PEG 400 on the properties of films formed after spraying was assessed. Its anti-inflammatory effect in mice was evaluated and compared to a commercial product. As the PEG 400 concentration increased, the film elongation and washability by the saliva solution increased, and tensile strength decreased. PEG 400 had little effect on mucoadhesive force and drug release. The TAA-loaded spray solution containing TAA, Eudragit L, PEG 400 and ethanol at the ratio of 1:6:3:100 (w/w/w/v) was easy to spray onto stomatitis lesions in the mouth via a spraying vessel incorporating a long straw. After spraying, the TAA-loaded spray formed a film with suitable elongation, tensile strength and washability that attached onto the mucosal membrane and released the drug. Moreover, it had excellent anti-inflammatory properties, similar to those of the commercial product. Thus, this novel TAA-loaded spray solution was easy to administer, had good film properties and excellent anti-inflammatory efficacy, and is therefore a potential candidate for the treatment of stomatitis.
( Rehmana Rashid ),( Dong Wuk Kim ),( Abid Mehmood Yousaf ),( Omer Mustapha ),( Fakhar Ud Din ),( Jong Hyuck Park ),( Chul Soon Yong ),( Yu Kyoung Oh ),( Yu Seok Youn ),( Jong Oh Kim ),( Han Gon Choi 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
Background: The objective of this study was to compare the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezetimibe-Ioaded solid self-nanoemulsifying drug delivery system (SNEDDS), surface modified solid dispersion (SMSD), and solvent evaporated solid dispersion (SESD) to identify the best drug delivery system with the highest oral bioavailability. Methods: For the liquid SNEDDS formulation, Capryol 90, Cremophor EL, and Tween 80 were selected as the oil, surfactant, and cosurfactant, respectively. The nanoemulsion-forming region was sketched using a pscudotemary phase diagram on the basis of reduced emulsion size. The optimized liquid SNEDDS was converted to solid SNEDDS by spray drying with silicon dioxide. Furthermore, SMSDs were prepared using the spray drying technique with various amounts of hydroxypropylcellulose and Tween 80, optimized on the basis of their drug solubility. The SESD formulation was prepared with the same composition of optimized SMSD. The aqueous solubility, dissolution, physicochemical properties, and pharmacokinetics of all of the formulations were investigated and compared with the drug powder. Results: The drug existed in the crystalline form in SMSD, but was changed into an amor-phous form in SNEDDS and SESD, giving particle sizes of approximately 24, 6, and 11 urn, respectively. All of these formulations significantly improved the aqueous solubility and dis-solution in the order of solid SNEDDS "``: SESD > SMSD, and showed a total higher plasma concentration than did the drug powder. Moreover, SESD gave a higher area under the drug concentration time curve from zero to infinity than did SNEDDS and SMSD, even if they were not significantly different, suggesting more improved oral bioavailability. Conclusion: Among the various formulations tested in this study, the SESD system would be strongly recommended as a drug delivery system for the oral administration of ezetimibe with poor water solubility.
Potential of nanoparticulate carriers for improved drug delivery via skin
Jin‑Ki Kim,Alam Zeb,Sadia Tabassam Arif,Maimoona Malik,Fawad Ali Shah,Fakhar Ud Din,Omer Salman Qureshi,Eun‑Sun Lee,Gwan‑Yeong Lee 한국약제학회 2019 Journal of Pharmaceutical Investigation Vol.49 No.5
Skin as a delivery route for drugs has attracted a great attention in recent decades as it avoids many of the limitations of oral and parenteral administration. However, the excellent barrier property of skin is a major obstacle in the effective transport of drugs through this route. The topmost layer of skin, the “stratum corneum” is the tightest one and is responsible for most of the resistance offered. This necessitates breaching the resistance of the stratum corneum reversibly and transiently in order to achieve a therapeutically meaningful level in systemic circulation or local skin. In last few decades, a number of approaches have been developed to improve the limited drug permeability through stratum corneum. One promising approach is the use of nanoparticulate carriers as they not only facilitate drug delivery across skin but also avoid the drawbacks of conventional skin formulations. This review focuses on nanoparticulate carriers including conventional liposomes, deformable liposomes, ethosomes, niosomes and lipid nanoparticles developed for topical and transdermal drug delivery. A special emphasis is placed on their composition, structure, mechanism of penetration and recent application. The presented data demonstrate the potential of these nanoparticulate carriers for dermal and transdermal delivery.
Rizvi, Syed Zaki Husain,Shah, Fawad Ali,Khan, Namrah,Muhammad, Iftikhar,Ali, Khan Hashim,Ansari, Muhammad Mohsin,Din, Fakhar ud,Qureshi, Omer Salman,Kim, Kyoung-Won,Choe, Yeong-Hwan,Kim, Jin-Ki,Zeb, A Elsevier 2019 International journal of pharmaceutics Vol.560 No.-
<P><B>Abstract</B></P> <P>The objective of current study was to develop solid lipid nanoparticles-loaded with simvastatin (SIM-SLNs) and investigate their <I>in vivo</I> anti-hyperlipidemic activity in poloxamer-induced hyperlipidemia model. Nano-template engineering technique was used to prepare SIM-SLNs with palmityl alcohol as lipid core and a mixture of Tween 40/Span 40/Myrj 52 to stabilize the core. The prepared SIM-SLNs were evaluated for physicochemical parameters including particle diameter, surface charge, morphology, incorporation efficiency, thermal behaviour and crystallinity. <I>In vitro</I> release profile of SIM-SLNs in simulated gastric and intestinal fluids was evaluated by using dialysis bag technique and anti-hyperlipidemic activity was assessed in hyperlipidemia rat model. SIM-SLNs revealed uniform particle size with spherical morphology, zeta potential of −24.9 mV and high incorporation efficiency (∼85%). Thermal behaviour and crystallinity studies demonstrated successful incorporation of SIM in the lipid core and its conversion to amorphous form. SIM-SLNs demonstrated a sustained SIM release from the lipid core of nanoparticles. SIM-SLNs significantly reduced the elevated serum lipids as indicated by ∼3.9 and ∼1.5-times decreased total cholesterol compared to those of untreated control and SIM dispersion treated hyperlipidemic rats. In conclusion, SIM-SLNs showed a great promise for improving the therapeutic outcomes of SIM via its effective oral delivery.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>