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Development and physical characterization of polymer-fish oil bigel (hydrogel/oleogel) system as a transdermal drug delivery vehicle

Rehman K, Mohd Amin MC, Zulfakar MH

J Oleo Sci, 2014;63(10):961-70.
PMID: 25252741

Polymer-Fish oil bigel (hydrogel/oleogel colloidal mixture) was developed by using fish oil and natural (sodium alginate) and synthetic (hydroxypropyl methylcellulose) polymer for pharmaceutical purposes. The bigels were closely monitored and thermal, rheological and mechanical properties were compared with the conventional hydrogels for their potential use as an effective transdermal drug delivery vehicle. Stability of the fish oil fatty acids (especially eicosapentanoic acid, EPA and docosahexanoic acid, DHA) was determined by gas chromatography and the drug content (imiquimod) was assessed with liquid chromatography. Furthermore, in vitro permeation study was conducted to determine the capability of the fish oil-bigels as transdermal drug delivery vehicle. The bigels showed pseudoplastic rheological features, with excellent mechanical properties (adhesiveness, peak stress and hardness), which indicated their excellent spreadability for application on the skin. Bigels prepared with mixture of sodium alginate and fish oil (SB1 and SB2), and the bigels prepared with the mixture of hydroxypropyl methylcellulose and fish oil (HB1-HB3) showed high cumulative permeation and drug flux compared to hydrogels. Addition of fish oil proved to be beneficial in increasing the drug permeation and the results were statistically significant (p < 0.05, one-way Anova, SPSS 20.0). Thus, it can be concluded that bigel formulations could be used as an effective topical and transdermal drug delivery vehicle for pharmaceutical purposes.

Matched MeSH terms: Hypromellose Derivatives/chemistry*
Design of multi-particulate "Dome matrix" with sustained-release melatonin and delayed-release caffeine for jet lag treatment

Razali S, Bose A, Chong PW, Benetti C, Colombo P, Wong TW

Int J Pharm, 2020 Sep 25;587:119618.
PMID: 32673769 DOI: 10.1016/j.ijpharm.2020.119618

Multi-particulate Dome matrix with sustained-release melatonin and delayed-release caffeine was designed to restore jet lag sleep-wake cycle. The polymeric pellets were produced using extrusion-spheronization technique and fluid-bed coated when applicable. The compact and Dome module were produced by compressing pellets with cushioning agent. Dome matrix was assembly of modules with pre-determined compact formulation and drug release characteristics. The physicochemical and in vivo pharmacokinetics of delivery systems were examined. Melatonin loaded alginate/chitosan-less matrix exhibited full drug release within 8 h gastrointestinal transit with low viscosity hydroxypropymethylcellulose as cushioning agent. The cushioning agent reduced burst drug release and omission of alginate-chitosan enabled full drug release. Delayed-release alginate-chitosan caffeine matrix was not attainable through polymer coating due to premature coat detachment. Admixing of cushioning agent high viscosity hydroxypropylmethylcellulose and high viscosity ethylcellulose (9:1 wt ratio) with coat-free caffeine loaded particulates introduced delayed-release response via hydroxypropylmethylcellulose swelled in early dissolution phase and ethylcellulose sustained matrix hydrophobicity at prolonged phase. The caffeine was released substantially in colonic fluid in response to matrix polymers being degraded by rat colonic content. Dome matrix with dual drug release kinetics and modulated pharmacokinetics is produced to introduce melatonin-induced sleep phase then caffeine-stimulated wake phase.

Matched MeSH terms: Hypromellose Derivatives
Polymeric films as vehicle for buccal delivery: swelling, mechanical, and bioadhesive properties

Peh KK, Wong CF

J Pharm Pharm Sci, 1999 May-Aug;2(2):53-61.
PMID: 10952770

To investigate the suitability of an SCMC (sodium carboxymethyl cellulose/polyethylene glycol 400/carbopol 934P) and an HPMC (hydroxypropylmethyl cellulose/polyethylene glycol 400/carbopol 934P) films as drug vehicle for buccal delivery.

Matched MeSH terms: Hypromellose Derivatives
In vitro controlled release of alfuzosin hydrochloride using HPMC-based matrix tablets and its comparison with marketed product

Nair A, Gupta R, Vasanti S

Pharm Dev Technol, 2007;12(6):621-5.
PMID: 18161635

The present study is an attempt to formulate a controlled-release matrix tablet formulation for alfuzosin hydrochloride by using low viscous hydroxy propyl methyl cellulose (HPMC K-100 and HPMC 15cps) and its comparison with marketed product. Different batches of tablets containing 10 mg of alfuzosin were prepared by direct compression technique and evaluated for their physical properties, drug content, and in vitro drug release. All the formulations had a good physical integrity, and the drug content between the batches did not vary by more than 1%. Drug release from the matrix tablets was carried out for 12 hr and showed that the release rate was not highly significant with different ratios of HPMC K-100 and HPMC15cps. Similar dissolution profiles were observed between formulation F3 and the marketed product throughout the study period. The calculated regression coefficients showed a higher r2 value with zero-order kinetics and Higuchi model in all the cases. Although both the models could be applicable, zero-order kinetics seems to be better. Hence, it can be concluded that the use of low viscous hydrophilic polymer of different grades (HPMC K-100 and HPMC 15cps) can control the alfuzosin release for a period of 12 hr and was comparable to the marketed product.

Matched MeSH terms: Hypromellose Derivatives
Characterization of hydroxypropylmethylcellulose films using microwave non-destructive testing technique

Anuar NK, Wui WT, Ghodgaonkar DK, Taib MN

J Pharm Biomed Anal, 2007 Jan 17;43(2):549-57.
PMID: 16978823

The applicability of microwave non-destructive testing (NDT) technique in characterization of matrix property of pharmaceutical films was investigated. Hydroxypropylmethylcellulose and loratadine were selected as model matrix polymer and drug, respectively. Both blank and drug loaded hydroxypropylmethylcellulose films were prepared using the solvent-evaporation method and were conditioned at the relative humidity of 25, 50 and 75% prior to physicochemical characterization using microwave NDT technique as well as ultraviolet spectrophotometry, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) techniques. The results indicated that blank hydroxypropylmethylcellulose film exhibited a greater propensity of polymer-polymer interaction at the O-H and C-H domains of the polymer chains upon conditioned at a lower level of relative humidity. In the case of loratadine loaded films, a greater propensity of polymer-polymer and/or drug-polymer interaction via the O-H moiety was mediated in samples conditioned at the lower level of relative humidity, and via the C-H moiety when 50% relative humidity was selected as the condition for sample storage. Apparently, the absorption and transmission characteristics of both blank and drug loaded films for microwave varied with the state of polymer-polymer and/or drug-polymer interaction involving the O-H and C-H moieties. The measurement of microwave NDT test at 8GHz was sensitive to the chemical environment involving O-H moiety while it was greatly governed by the C-H moiety in test conducted at a higher frequency band of microwave. Similar observation was obtained with respect to the profiles of microwave NDT measurements against the state of polymer-polymer and/or drug-polymer interaction of hydroxypropylmethylcellulose films containing chlorpheniramine maleate. The microwave NDT measurement is potentially suitable for use as an apparent indicator of the state of polymer-polymer and drug-polymer interaction of the matrix.

Matched MeSH terms: Hypromellose Derivatives
Fulltext Synthesis and Characterization of Nanohydroxyapatite-Gelatin Composite with Streptomycin as Antituberculosis Injectable Bone Substitute

Hikmawati D, Maulida HN, Putra AP, Budiatin AS, Syahrom A

Int J Biomater, 2019;2019:7179243.
PMID: 31341479 DOI: 10.1155/2019/7179243

The most effective treatment for spinal tuberculosis was by eliminating the tuberculosis bacteria and replacing the infected bone with the bone graft to induce the healing process. This study aims to synthesize and characterize nanohydroxyapatite-gelatin-based injectable bone substitute (IBS) with addition of streptomycin. The IBS was synthesized by mixing nanohydroxyapatite and 20 w/v% gelatin with ratio of 40:60, 45:55, 50:50, 55:45, 60:40, 65:35, 70:30, and 75:25 ratio and streptomycin addition as antibiotic agent. The mixture was added by hydroxypropyl methylcellulose as suspending agent. FTIR test showed that there was a chemical reaction occurring in the mixture, between the gelatin and streptomycin. The result of injectability test showed that the highest injectability of the IBS sample was 98.64% with the setting time between 30 minutes and four hours after injection on the HA scaffold that represents the bone cavity and coat the pore scaffold. The cytotoxicity test result showed that the IBS samples were nontoxic towards BHK-21 fibroblast cells and human hepatocyte cells since the viability cell was more than 50% with significant difference (p-value<0.05). The acidity of the IBS was stable and it was sensitive towards Staphylococcus aureus with significantly difference (p-value<0.05). The streptomycin release test showed that the streptomycin could be released from the IBS-injected bone scaffold with release of 2.5% after 4 hours. All the results mentioned showed that IBS was suitable as a candidate to be used in spinal tuberculosis case.

Matched MeSH terms: Hypromellose Derivatives
Fulltext In situ ophthalmic gel forming systems of poloxamer 407 and hydroxypropyl methyl cellulose mixtures for sustained ocular delivery of chloramphenicole: optimization study by factorial design

Kurniawansyah IS, Rusdiana T, Sopyan I, Ramoko H, Wahab HA, Subarnas A

Heliyon, 2020 Nov;6(11):e05365.
PMID: 33251348 DOI: 10.1016/j.heliyon.2020.e05365

Background: Conventional drug delivery systems have some major drawbacks such as low bioavailability, short residence time and rapid precorneal drainage. An in situ gel drug delivery system provides several benefits, such as prolonged pharmacological duration of action, simpler production techniques, and low cost of manufacturing. This research aims to get the optimum formula of chloramphenicol in situ gel based on the physical evaluation.
Methods: The effects of independent variables (poloxamer 407 and hydroxypropyl methyl cellulose (HPMC) concentration) on various dependent variables (gelling capacity, pH and viscosity) were investigated by using 32 factorial design and organoleptic evaluation was done with descriptive analysis.
Results: The optimized formula of chloramphenicol in situ gel yielded 9 variations of poloxamer 407 and HPMC bases composition in % w/v as follows, F1 (5; 0.45), F2 (7.5; 0.45), F3 (10; 0.45), F4 (5; 0.725), F5 (7.5; 0.725), F6 (10; 0.725), F7 (5; 1), F8 (7.5; 1), F9 (10; 1). The results indicated that the organoleptic, pH, and gelling capacity parameters matched all formulas (F1-F9), however, the viscosity parameter only matched F3, F6, F8, and F9. Based on factorial design, F6 had the best formula with desirability value of 0.54, but the design recommended that formula with the composition bases of poloxamer 407 and HPMC at the ratio of 8.16 % w/v and 0.77 % w/v, respectively, was the optimum formula with a desirability value of 0.69.
Conclusion: All formulas have met the Indonesian pharmacopoeia requirements based on the physical evaluation, especially formula 6 (F6), which was supported by the result of factorial design analysis.

Matched MeSH terms: Hypromellose Derivatives
In vitro and in vivo evaluation of hydrophilic and hydrophobic polymers-based nicorandil-loaded peroral tablet compared with its once-daily commercial sustained-release tablet

Tamilvanan S, Venkatesh Babu R, Nappinai A, Sivaramakrishnan G

Drug Dev Ind Pharm, 2011 Apr;37(4):436-45.
PMID: 20923389 DOI: 10.3109/03639045.2010.521161

Hydrophilic and hydrophobic polymer-based nicorandil (10 mg)-loaded peroral tablets were prepared using the wet granulation technique. The influence of varying amounts of hydroxypropyl methylcellulose (HPMC) (30-50 mg), ethylcellulose (2-4 mg), microcrystalline cellulose (5-20 mg) and Aerosil® (5-12 mg) in conjunction with the constant amounts (3 mg) of glidant and lubricant (magnesium stearate and talc) on the in vitro performances of the tablets (hardness, friability, weight variation, thickness uniformity, drug content, and drug release behavior) were investigated.

Matched MeSH terms: Hypromellose Derivatives
Fulltext Formulation development and optimization of sustained release matrix tablet of Itopride HCl by response surface methodology and its evaluation of release kinetics

Bose A, Wong TW, Singh N

Saudi Pharm J, 2013 Apr;21(2):201-13.
PMID: 23960836 DOI: 10.1016/j.jsps.2012.03.006

The objective of this present investigation was to develop and formulate sustained release (SR) matrix tablets of Itopride HCl, by using different polymer combinations and fillers, to optimize by Central Composite Design response surface methodology for different drug release variables and to evaluate drug release pattern of the optimized product. Sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: hydroxy propyl methyl cellulose (HPMC) and polyvinyl pyrolidine (pvp) and lactose as fillers. Study of pre-compression and post-compression parameters facilitated the screening of a formulation with best characteristics that underwent here optimization study by response surface methodology (Central Composite Design). The optimized tablet was further subjected to scanning electron microscopy to reveal its release pattern. The in vitro study revealed that combining of HPMC K100M (24.65 MG) with pvp(20 mg)and use of LACTOSE as filler sustained the action more than 12 h. The developed sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.

Matched MeSH terms: Hypromellose Derivatives
Fulltext Formulation of aerosol concentrates containing haruan (Channa striatus) for wound dressing

Febriyenti, Azmin Mohd. Noor, Saringat Baei

Malaysian Journal of Pharmaceutical Science, 2008;6(1):43-58.
MyJurnal

The objective of this research was to formulate an aerosol concentrate containing haruan (Channa
striatus) water extract that would produce a thin film when sprayed onto a wound and could be used for wound dressing. The aerosol concentrates were formulated with various polymer and plasticiser mixtures and tested in dispersion systems. The polymers evaluated were hydroxypropyl methylcellulose (HPMC), carboxymethylcellulose sodium (CMC Sodium), acacia, tragacanth, chitosan, gelatine and gelatine (bloom 151–160), all at concentrations of 2%. The plasticisers evaluated were polyethylene glycol (PEG) 400 and 4000, glycerine, propylene glycol, and triacetin. Films were prepared from film-forming dispersions by casting techniques. Film-forming dispersions were characterised in terms of pH, density, surface tension, rheological properties, particle size distribution, and tackiness. Based on these evaluations, HPMC was chosen as the best polymer. It produced a film with the expected qualities and was easy to reproduce in the form of dispersions or as thin transparent films. Glycerine was judged as the most appropriate plasticiser because it produced the concentrate having the desired qualities and properties expected from an aerosol concentrate.

Matched MeSH terms: Hypromellose Derivatives
Aceclofenac topical dosage forms: in vitro and in vivo characterization

Dua K, Pabreja K, Ramana MV

Acta Pharm, 2010 Dec;60(4):467-78.
PMID: 21169138 DOI: 10.2478/v1007-010-0036-5

Aceclofenac is a new generation non-steroidal anti-inflammatory drug showing effective anti-inflammatory and analgesic properties. It is available in the form of tablets of 100 mg. Importance of aceclofenac as a NSAID has inspired development of topical dosage forms. This mode of administration may help avoid typical side effects associated with oral administration of NSAIDs, which have led to its withdrawal. Furthermore, aceclofenac topical dosage forms can be used as a supplement to oral therapy for better treatment of conditions such as arthritis. Ointments, creams, and gels containing 1% (m/m) aceclofenac have been prepared. They were tested for physical appearance, pH, spreadability, extrudability, drug content uniformity, in vitro diffusion and in vitro permeation. Gels prepared using Carbopol 940 (AF2, AF3) and macrogol bases (AF7) were selected after the analysis of the results. They were evaluated for acute skin irritancy, anti-inflammatory and analgesic effects using the carrageenan-induced thermal hyperalgesia and paw edema method. AF2 was shown to be significantly (p < 0.05) more effective in inhibiting hyperalgesia associated with inflammation, compared to AF3 and AF7. Hence, AF2 may be suggested as an alternative to oral preparations.

Matched MeSH terms: Hypromellose Derivatives
Effect of HPMC concentration on β-cyclodextrin solubilization of norfloxacin

Loh GO, Tan YT, Peh KK

Carbohydr Polym, 2014 Jan 30;101:505-10.
PMID: 24299805 DOI: 10.1016/j.carbpol.2013.09.084

The effect of hydroxypropyl methylcellulose (HPMC) concentration on β-cyclodextrin (β-CD) solubilization of norfloxacin was examined. The solubility and dissolution of norfloxacin/β-CD and norfloxacin/β-CD/HPMC inclusion complexes were studied. The presence of β-CD increased significantly the solubility and dissolution of norfloxacin. The addition of HPMC until 5% (w/w) improved the solubilization of norfloxacin but further addition above 5% (w/w), decreased norfloxacin solubilization. Fourier transformed Infra-red (FTIR) showed that norfloxacin was successfully included into β-CD. Differential scanning calorimetry (DSC) showed that the norfloxacin endothermic peak shifted to a lower temperature with reduced intensity indicating the formation of inclusion complex. The addition of HPMC reduced further the intensity of norfloxacin endothermic peak. Most of the sharp and intense peaks of norfloxacin disappeared with the addition of HPMC. In conclusion, the concentration of hydrophilic polymer used to enhance β-CD solubilization of poorly soluble drugs is very critical.

Matched MeSH terms: Hypromellose Derivatives
Investigation on the effect of polymer and starch on the tablet properties of lyophilized orally disintegrating tablet

Liew KB, Peh KK

Arch Pharm Res, 2021 Aug;44(8):1-10.
PMID: 25579848 DOI: 10.1007/s12272-014-0542-y

Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.

Matched MeSH terms: Hypromellose Derivatives/chemistry
Fulltext Continuous Monitoring of the Hydration Behavior of Hydrophilic Matrix Tablets Using Time-Domain NMR

Tsuji T, Ono T, Taguchi H, Leong KH, Hayashi Y, Kumada S, et al.

Chem Pharm Bull (Tokyo), 2023;71(7):576-583.
PMID: 37394606 DOI: 10.1248/cpb.c23-00214

Time-domain NMR (TD-NMR) was used for continuous monitoring of the hydration behavior of hydrophilic matrix tablets. The model matrix tablets comprised high molecular weight polyethylene oxide (PEO), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG). The model tablets were immersed in water. Their T2 relaxation curves were acquired by TD-NMR with solid-echo sequence. A curve-fitting analysis was conducted on the acquired T2 relaxation curves to identify the NMR signals corresponding to the nongelated core remaining in the samples. The amount of nongelated core was estimated from the NMR signal intensity. The estimated values were consistent with the experiment measurement values. Next, the model tablets immersed in water were monitored continuously using TD-NMR. The difference in hydration behaviors of the HPMC and PEO matrix tablets was then characterized fully. The nongelated core of the HPMC matrix tablets disappeared more slowly than that of the PEO matrix tablets. The behavior of HPMC was significantly affected by the PEG content in the tablets. It is suggested that the TD-NMR method has potential to be utilized to evaluate the gel layer properties, upon replacement of the immersion medium: purified (nondeuterated) water is replaced with heavy (deuterated) water. Finally, drug-containing matrix tablets were tested. Diltiazem hydrochloride (a highly water-soluble drug) was employed for this experiment. Reasonable in vitro drug dissolution profiles, which were in accordance with the results from TD-NMR experiments, were observed. We concluded that TD-NMR is a powerful tool to evaluate the hydration properties of hydrophilic matrix tablets.

Matched MeSH terms: Hypromellose Derivatives/chemistry
Fulltext Formulation and in vitro, in vivo evaluation of effervescent floating sustained-release imatinib mesylate tablet

Kadivar A, Kamalidehghan B, Javar HA, Davoudi ET, Zaharuddin ND, Sabeti B, et al.

PLoS One, 2015;10(6):e0126874.
PMID: 26035710 DOI: 10.1371/journal.pone.0126874

Imatinib mesylate is an antineoplastic agent which has high absorption in the upper part of the gastrointestinal tract (GIT). Conventional imatinib mesylate (Gleevec) tablets produce rapid and relatively high peak blood levels and requires frequent administration to keep the plasma drug level at an effective range. This might cause side effects, reduced effectiveness and poor therapeutic management. Therefore, floating sustained-release Imatinib tablets were developed to allow the tablets to be released in the upper part of the GIT and overcome the inadequacy of conventional tablets.

Matched MeSH terms: Hypromellose Derivatives/chemistry
Fulltext Effect of some biopolymers on the rheological behavior of surimi gel

Sarker ZI, Elgadir MA, Ferdosh S, Akanda JH, Manap MY, Noda T

Molecules, 2012;17(5):5733-44.
PMID: 22628045 DOI: 10.3390/molecules17055733

The objective of this study was to investigate the effect of selected biopolymers on the rheological properties of surimi. In our paper, we highlight the functional properties and rheological aspects of some starch mixtures used in surimi. However, the influence of some other ingredients, such as cryoprotectants, mannans, and hydroxylpropylmethylcellulose (HPMC), on the rheological properties of surimi is also described. The outcome reveals that storage modulus increased with the addition of higher levels of starch. Moreover, the increasing starch level increased the breaking force, deformation, and gel strength of surimi as a result of the absorption of water by starch granules in the mixture to make the surimi more rigid. On the other hand, the addition of cryoprotectants, mannans, and HPMC improved the rheological properties of surimi. The data obtained in this paper could be beneficial particularly to the scientists who deal with food processing field.

Matched MeSH terms: Hypromellose Derivatives
The influence of different plasticizers on some physical and mechanical properties of hydroxypropyl methylcellulose free films

Saringat HB, Alfadol KI, Khan GM

Pak J Pharm Sci, 2005 Jul;18(3):25-38.
PMID: 16380341

Coating has been widely used in pharmaceutical manufacture either as non-functional or a functional entity. The objectives of the present study were to investigate the effect of plasticizers such as PEG400, PEG1000 and triacetin on mechanical properties, glass transition temperature and water vapor transmission of free films prepared from HPMC and/or HPMC:PVA blends, to develop suitable coating system for tablets, and to determine the release profiles of the coated tablets. The tensile strength of plasticized HPMC films was generally lower than that of control HPMC film and could be attributed to increased crystallinity and segmental chain mobility of HPMC. This effect increased as the concentration of plasticizer increased. Generally the addition of both grades of polyethylene glycol (PEG400 & PEG1000) increased the moisture permeability of HPMC films but the films containing triacetin provided a more rigid barrier to moisture compared to unplasticized HPMC films. The dissolution profiles of paracetamol tablets coated with 7% w/v HPMC coating-solutions containing PEG400, PEG1000 and triacetin, and those containing PEG400 & PVA together showed that HPMC had weak water resistance. The presence of PEG400 and 1000 in HPMC films further weakened its resistance to solubility while the presence of triacetin caused a little increase in HPMC water resistance. From the results it was concluded that HPMC at 7%w/w concentration was suitable for film-coating intended for non-functional coating. Presence of the PEG 400, PEG1000 and triacetin as well as the presence of PVA and PEG400 together improved the coating properties of HPMC films and made it more suitable as a non-functional coating material.

Matched MeSH terms: Hypromellose Derivatives
Smart nanocrystals of artemether: fabrication, characterization, and comparative in vitro and in vivo antimalarial evaluation

Shah SM, Ullah F, Khan S, Shah SM, de Matas M, Hussain Z, et al.

Drug Des Devel Ther, 2016;10:3837-3850.
PMID: 27920499

Artemether (ARTM) is a very effective antimalarial drug with poor solubility and consequently low bioavailability. Smart nanocrystals of ARTM with particle size of 161±1.5 nm and polydispersity index of 0.172±0.01 were produced in <1 hour using a wet milling technology, Dena(®) DM-100. The crystallinity of the processed ARTM was confirmed using differential scanning calorimetry and powder X-ray diffraction. The saturation solubility of the ARTM nanocrystals was substantially increased to 900 µg/mL compared to the raw ARTM in water (145.0±2.3 µg/mL) and stabilizer solution (300.0±2.0 µg/mL). The physical stability studies conducted for 90 days demonstrated that nanocrystals stored at 2°C-8°C and 25°C were very stable compared to the samples stored at 40°C. The nanocrystals were also shown to be stable when processed at acidic pH (2.0). The solubility and dissolution rate of ARTM nanocrystals were significantly increased (P<0.05) compared to those of its bulk powder form. The results of in vitro studies showed significant antimalarial effect (P<0.05) against Plasmodium falciparum and Plasmodium vivax. The IC50 (median lethal oral dose) value of ARTM nanocrystals was 28- and 54-fold lower than the IC50 value of unprocessed drug and 13- and 21-fold lower than the IC50 value of the marketed tablets, respectively. In addition, ARTM nanocrystals at the same dose (2 mg/kg) showed significantly (P<0.05) higher reduction in percent parasitemia (89%) against P. vivax compared to the unprocessed (27%), marketed tablets (45%), and microsuspension (60%). The acute toxicity study demonstrated that the LD50 value of ARTM nanocrystals is between 1,500 mg/kg and 2,000 mg/kg when given orally. This study demonstrated that the wet milling technology (Dena(®) DM-100) can produce smart nanocrystals of ARTM with enhanced antimalarial activities.

Matched MeSH terms: Hypromellose Derivatives/chemistry
Domperidone nanocrystals with boosted oral bioavailability: fabrication, evaluation and molecular insight into the polymer-domperidone nanocrystal interaction

Ndlovu ST, Ullah N, Khan S, Ramharack P, Soliman M, de Matas M, et al.

Drug Deliv Transl Res, 2019 Feb;9(1):284-297.
PMID: 30387048 DOI: 10.1007/s13346-018-00596-w

The aim of this study was to employ experimental and molecular modelling approaches to use molecular level interactions to rationalise the selection of suitable polymers for use in the production of stable domperidone (DOMP) nanocrystals with enhanced bioavailability. A low-energy antisolvent precipitation method was used for the preparation and screening of polymers for stable nanocrystals of DOMP. Ethyl cellulose was found to be very efficient in producing stable DOMP nanocrystals with particle size of 130 ± 3 nm. Moreover, the combination of hydroxypropyl methylcellulose and polyvinyl alcohol was also shown to be better in producing DOMP nanocrystals with smaller particle size (200 ± 3.5 nm). DOMP nanosuspension stored at 2-8 °C and at room temperature (25 °C) exhibited better stability compared to the samples stored at 40 °C. Crystallinity of the unprocessed and processed DOMP was monitored by differential scanning calorimetry and powder X-ray diffraction. DOMP nanocrystals gave enhanced dissolution rate compared to the unprocessed drug substance. DOMP nanocrystals at a dose of 10 mg/kg in rats showed enhanced bioavailability compared to the raw drug substance and marketed formulation. A significant increase in plasma concentration of 2.6 μg/mL with a significant decrease in time (1 h) to reach maximum plasma concentration was observed for DOMP nanocrystals compared to the raw DOMP. Molecular modelling studies provided underpinning knowledge at the molecular level of the DOMP-polymer nanocrystal interactions and substantiated the experimental studies. This included an understanding of the impact of polymers on the size of nanocrystals and their associated stability characteristics.

Matched MeSH terms: Hypromellose Derivatives/chemistry*
Fulltext Dataset on applying HPMC polymer to improve encapsulation efficiency and stability of the fish oil: In vitro evaluation

Zaidul ISM, Fahim TK, Sahena F, Azad AK, Rashid MA, Hossain MS

Data Brief, 2020 Oct;32:106111.
PMID: 32904423 DOI: 10.1016/j.dib.2020.106111

Data examines the effect of hydroxypropyl methylcellulose (HPMC) HPMC15 cP, and HPMC 5 cP polymer composition on the physicochemical traits of encapsulated oil made using lab scale spray drying (180 °C). The data found showed that the properties of the reconstituted fish oil powder are significantly affected by the polymer's composition and ratio (p < 0.05). In this experiment, powder with the particle sizes below 60 μm was produced and it was observed that HPMC is a good emulsifier for all formulations and the encapsulation efficiency is high with 75.21% for AF1 formulation. It was also observed that the process of fish oil encapsulation employed by HPMC 5 cP produce a more volatile oil powder, while encapsulation with HPMC 15 cP produced a more stable fish oil powder. These finding shows that the utilisation of HPMC as a polymer to encapsulate fish oil can produce a more efficient and stable compound.

Matched MeSH terms: Hypromellose Derivatives

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