Hydroxypropyl Methylcellulose Phthalate Research Articles

Modified Release 3D-Printed Capsules Containing a Ketoprofen Self-Nanoemulsifying System for Personalized Medical Application.

This study explores the realm of personalized medicine by investigating the utilization of 3D-printed dosage forms, specifically focusing on patient-specific enteric capsules designed for the modified release of ketoprofen, serving as a model drug. The research investigates two distinct scenarios: the modification of drug release from 3D-printed capsules crafted from hydroxypropyl methylcellulose phthalate:polyethylene glycol (HPMCP:PEG) and poly(vinyl alcohol) (PVA), tailored for pH sensitivity and delayed release modes, respectively. Additionally, a novel ketoprofen-loaded self-nanoemulsifying drug delivery system (SNEDDS) based on pomegranate seed oil (PSO) was developed, characterized, and employed as a fill material for the capsules. Through the preparation and characterization of the HPMCP:PEG based filament via the hot-melt extrusion method, the study thoroughly investigated its thermal and mechanical properties. Notably, the in vitro drug release analysis unveiled the intricate interplay between ketoprofen release, polymer type, and capsule thickness. Furthermore, the incorporation of ketoprofen into the SNEDDS exhibited an enhancement in its in vitro cylooxygenase-2 (COX-2) inhibitory activity. These findings collectively underscore the potential of 3D printing in shaping tailored drug delivery systems, thereby contributing significantly to the advancement of personalized medicine.

Hydrolysis of Cellulose Acetate Phthalate and Hydroxypropyl Methylcellulose Phthalate in Amorphous Solid Dispersions

The preparation of amorphous solid dispersions (ASDs) represents a promising strategy for addressing the solubility limitations of poorly soluble drugs, facilitating enhanced absorption. Acidic polymers such as cellulose acetate phthalate (CAP) and hydroxypropyl methylcellulose phthalate (HPMCP) have emerged as effective carriers for ASDs. Although the hydrolytic degradation of these polymers has been documented, its impact on the stability of ASDs has not been systematically investigated. This research aimed to explore the potential hydrolysis of CAP and HPMCP and how it influences the stability of ASDs containing ketoconazole (KTZ), at drug loadings of 10 % and 50 %. Our study utilized thermal analysis, infrared spectroscopy, and evaluations of physical and chemical stability. The results revealed that although KTZ remained physically stable in all ASDs over a 60-day period under various stability conditions, the emergence of crystalline phthalic acid (PA), a byproduct of polymer hydrolysis, was observed at elevated temperatures and relative humidity levels. The acidic microenvironment fostered by the release of PA further catalyzed drug chemical degradation. This study underscores the susceptibility of CAP and HPMCP to hydrolytic degradation, highlighting the inherent risk of PA-induced drug degradation, particularly for acid-labile compounds. These insights into the understanding of polymer hydrolysis in ASDs pave the way for the development of targeted approaches to safeguard drug stability and optimize pharmaceutical formulations for enhanced bioavailability, efficacy, and safety.

Comparison of the protective effects of CS/TPP and CS/HPMCP nanoparticles containing berberine in ethanol-induced hepatotoxicity in rat

BackgroundAlcoholic liver disease (ALD) is a globally critical condition with no available efficient treatments.MethodsHerein, we generated chitosan (CS) nanoparticles cross-linked with two different agents, hydroxypropyl methylcellulose phthalate (HPMCP; termed as CS/HPMCP) and tripolyphosphate (TPP; termed as CS/TPP), and loaded them with berberine (BBr; referred to as CS/HPMCP/BBr and CS/TPP/BBr, respectively). Alongside the encapsulation efficiency (EE) and loading capacity (LC), the releasing activity of the nanoparticles was also measured in stimulated gastric fluid (SGF) and stimulated intestinal fluid (SIF) conditions. The effects of the prepared nanoparticles on the viability of mesenchymal stem cells (MSCs) were also evaluated. Ultimately, the protective effects of the nanoparticles were investigated in ALD mouse models.ResultsSEM images demonstrated that CS/HPMCP and CS/TPP nanoparticles had an average size of 235.5 ± 42 and 172 ± 21 nm, respectively. The LC and EE for CS/HPMCP/BBr were calculated as 79.78% and 75.79%, respectively; while the LC and EE for CS/TPP/BBr were 84.26% and 80.05%, respectively. pH was a determining factor for releasing BBr from CS/HPMCP nanoparticles as a higher cargo-releasing rate was observed in a less acidic environment. Both the BBr-loaded nanoparticles increased the viability of MSCs in comparison with their BBr-free counterparts. In vivo results demonstrated CS/HPMCP/BBr and CS/TPP/BBr nanoparticles protected enzymatic liver functionality against ethanol-induced damage. They also prevented histopathological ethanol-induced damage.ConclusionsCrosslinking CS nanoparticles with HPMCP can mediate controlled drug release in the intestine improving the bioavailability of BBr.

PH-responsive mesoporous silica nanorod for high load and oral delivery of insulin

Diabetes is a metabolic disease often characterized by elevated blood sugar levels, which is mainly treated through external injection of insulin. However, long-term insulin injection in patients will produce many adverse side effects such as hypoglycemia, subcutaneous fat atrophy and prolonged absorption, resulting in poor patient compliance. In this work, mesoporous silica (SBA-15) nanorods with large surface area (541.8 m2/g) were prepared via soft-templating method, which retained a large number of ordered mesoporous structures as the drug delivery carrier for insulin. Insulin-loaded mesoporous silica (SBA-15/INS) particle was obtained by solvent adsorption, which was then coated with hydroxypropyl methylcellulose phthalate (HP55) to form pH-sensitive mesoporous silica nanoparticles (HP55@SBA-15/INS). The surface area, structure and morphology of silica particles were addressed by BET, FTIR, XRD, SEM and TEM, indicating that SBA-15/INS and HP55@SBA-15/INS maintained the rod-like and ordered white strips structure similar to SBA-15. Also, insulin was found to be present in the mesoporous silica nanoparticles, with loading capacity and encapsulation efficiency reaching 25.5 % and 80.9 %, respectively. The vitro release results revealed that insulin release in the simulated gastric fluid (SGF, pH = 1.2) was significantly slower than that in the simulated intestinal fluid (SIF, pH = 7.4). Compared with SBA-15/INS, the release percentages in 15 % HP55@SBA-15/INS decreased 30 % in SGF, while it increased approximately 10 % in SIF. Kinetics analysis showed that the release process in HP55@SBA-15/INS was a Fick diffusion in both SGF and SIF and HP55 was degraded in SIF, resulting in accelerated insulin release. The cytotoxicity evaluation results showed that the cell viability of 4T1 after 24 h incubated with SBA-15 and 15 % HP55@SBA-15/INS was both approximately 100 %, demonstrating that the facile manufactured method has great potential to prepare macromolecular drug nanoparticle for oral release.

Super Bioavailable (SUBA) Itraconazole-Induced Galactorrhea-Could it be due to Hydroxypropyl Methylcellulose Phthalate?

Super Bioavailable (SUBA) Itraconazole-Induced Galactorrhea-Could it be due to Hydroxypropyl Methylcellulose Phthalate?

Characterization and stability investigation of rhein encapsulated microcapsules using different enteric biopolymers with pullulan and Jiuzao glutelin conjugates via Maillard reaction

The poor water solubility and rhein (RH) stability limit its application in the functional food industry. In the present study, the RH-loaded water-in-oil-in-water nano emulsion and microcapsules were prepared using the conjugates of pullulan-Jiuzao glutelin (JG) (m/m, 2:1, PJC-2) obtained by Maillard reaction and enteric-soluble materials (polymethlacrylic acid, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, and D-mannitol). The effects of different formulations on the microstructure, physicochemical properties, and storage stability of microcapsules were analyzed. The results showed that microcapsules exhibited stability against different external environments. The encapsulation efficiency of RH in the four enteric-soluble-PJC-2 double-deck microcapsules (70.03 ± 3.24%-91.08 ± 4.78%) was significantly improved than PJC-2 ones (61.84 ± 0.47%). The antioxidant activity and stability of RH in the microcapsules were improved (ABTS, 49.7%-113.93%; DPPH, 40.85%-101.82%; FRA, 62.32%-126.42%; and FCA, 70.58%-147.20%) after in vitro simulated digestion and extreme environmental conditions compared to free RH. This work provides a microcapsule based on PJC-2 with enteric-soluble materials for insoluble functional ingredients to improve solubility, stability, and bioactivity in the food industry.

PH-sensitive HPMCP-chitosan nanoparticles containing 5-aminosalicylic acid and berberine for oral colon delivery in a rat model of ulcerative colitis

Ulcerative colitis (UC) with continuous and extensive inflammation is limited to the colon mucosa and can lead to abdominal pain, diarrhea, and rectal bleeding. Conventional therapies are associated with several limitations, such as systemic side effects, drug degradation, inactivation, and limited drug uptake, leading to poor bioavailability. These restrictions necessitate drug delivery to the colon so that the drug passes through the stomach unchanged and has selective access to the colon. The present study aimed to formulate 5-aminosalicylic acid (5-ASA) and berberine (BBR) in chitosan nanoparticles cross-linked by HPMCP (hydroxypropyl methylcellulose phthalate) as a colon drug delivery system for UC. Spherical nanoparticles were prepared. They showed appropriate drug release in the simulated intestinal fluid (SIF), while the release did not occur in the simulated gastric fluid (SGF). They improved disease activity parameters (DAI) and ulcer index, increased the length of the colon, and decreased the wet weight of the colon. Furthermore, histopathological colon studies showed an improved therapeutic effect of 5-ASA/HPMCP/CSNPs and BBR/HPMCP/CSNPs. In conclusion, although 5-ASA/HPMCP/CSNPs showed the best effect in the treatment of UC, BBR/HPMCP/CSNPs, and 5-ASA/BBR/HPMCP/CSNPs were also effective in vivo study, and this study anticipated they could be helpful in future clinical applications for the management of UC.

Synergistic effect of miscible cellulose-based microparticles and pH modulators on the bioavailability of a weakly basic drug and its metabolites

This study aimed to evaluate the miscibility of cellulose derivatives to improve the release rate and stability of microparticles containing the weakly basic drug itraconazole (ITZ). We also investigated the effect of some organic acids on the microenvironmental pH (pHm) and the release rate of ITZ from the cellulose-based microparticles. The synergistic effect of cellulose-based microparticles and pHm modulators on the bioavailability of ITZ compared with the reference product was investigated in a rabbit model. Differential scanning calorimetry and Fourier-transform infrared spectroscopy (FTIR) analysis showed that ITZ, hydroxypropyl methylcellulose, and hydroxypropyl methylcellulose phthalate were miscible at a ratio of 1.5:3:1 (w/w/w), and the stability of the microparticles was maintained for 6 months under accelerated conditions. In addition, X-ray diffraction, FTIR, and scanning electron microscopy were used to characterize the properties of the microparticles. Through the titration technique and determination of pHm, the combination of fumaric acid and maleic acid (1:2, w/w) was found to be the most effective pHm modulator for microparticles. The integration of cellulose-based microparticles and pHm modulators showed a synergistic effect on the flux and relative bioavailability of ITZ and its active metabolite OH-ITZ (182.60 % and 217.67 %, respectively) when compared with the reference product.

Impact of Gastric pH Variations on the Release of Amorphous Solid Dispersion Formulations Containing a Weakly Basic Drug and Enteric Polymers.

Enteric polymers are widely used in amorphous solid dispersion (ASD) formulations. The aim of the current study was to explore ASD failure mechanisms across a wide range of pH conditions that mimic in vivo gastric compartment variations where enteric polymers such as hydroxypropyl methylcellulose phthalate (HPMCP) and hydroxypropyl methylcellulose acetate succinate (HPMCAS) are largely insoluble. Delamanid (DLM), a weakly basic drug used to treat tuberculosis, was selected as the model compound. Both DLM free base and the edisylate salt were formulated with HPMCP, while DLM edisylate ASDs were also prepared with different grades of HPMCAS. Two-stage release testing was conducted with the gastric stage pH varied between pH 1.6 and 5.0, prior to transfer to intestinal conditions of pH 6.5. ASD particles were collected following suspension in the gastric compartment and evaluated using X-ray powder diffraction and scanning electron microscopy. Additional samples were also evaluated with polarized light microscopy. In general, ASDs with HPMCP showed improved overall release for all testing conditions, relative to ASDs with HPMCAS. ASDs with the edisylate salt likewise outperformed those with DLM free base. Impaired release for certain formulations at intestinal pH conditions was attributed to surface drug crystallization that initiated during suspension in the gastric compartment where the polymer is insoluble; crystallization appeared more extensive for HPMCAS ASDs. These findings suggest that gastric pH variations should be evaluated for ASD formulations containing weakly basic drugs and enteric polymers.

A developed composite hard-gelatin capsules: delayed-release enteric properties

Present study focused on improvement of the formulation of conventional hard gelatin capsules using gastric acid-resistant polymers. We have utilized the same approach of making conventional drug capsules to develop novel capsules with delayed release properties. For this purpose, delayed-release capsules were produced by improving the formulation of hard gelatin capsules. In addition, the effect of adding intestinal polymers such as Hydroxy propyl methyl cellulose phthalate, Glucomannan, and Polyvinyl alcohol to hard gelatin capsules were investigated. The capsules' release rate was determined. The degradation tests in an acidic environment were performed and the results were recorded. In fact, the delayed-release hard gelatin capsules pass through the stomach with small amount of the drug release; but their shell remains intact and dissolves as it enters the intestine environment.This article shows that enteric polymers with out interactions, only by changing the formulations will have delayed release properties. this makes sensitive drugs pass through stomach environment and have higher absorption.

Moisture Sorption by Polymeric Excipients Commonly Used in Amorphous Solid Dispersions and its Effect on Glass Transition Temperature: II. Cellulosic Polymers

Moisture sorption by polymeric carriers used for the development of amorphous solid dispersions (ASDs) plays a critical role in the physical stability of dispersed drugs since moisture may decrease glass transition temperature (Tg) and thereby increase molecular mobility of drugs leading to their crystallization. To assist the selection of appropriate polymers for ASDs, we conducted moisture sorption by five types of cellulosic polymers, namely, hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), hydroxypropyl methyl cellulose acetate succinate (HPMCAS), hydroxypropyl methyl cellulose phthalate (HPMCP), and ethyl cellulose (EC), as functions of relative humidity (10 to 90% RH) and temperature (25 and 40 °C). The moisture sorption was in the order of HPC>HPMC>HPMCP>HPMCAS>EC, and there was no significant effect of the molecular weights of polymers on moisture uptake. There was also less moisture sorption at 40 °C than that at 25 °C. Glass transition temperatures (Tg) of the polymers decreased with the increase in moisture content. However, the plasticizing effect by moisture on HPC could not be determined fully since, despite being amorphous, there were very little baseline shifts in DSC scans. There was also very shallow baseline shift for HPMC at >1% moisture content. In contrast, Tg of HPMCAS and HPMCP decreased in general agreement with the Gordon-Taylor/Kelley-Bueche equation, and EC was semicrystalline having both Tg and melting endotherm, with only minor effect of moisture on Tg. The results of the present investigation would lead to a systematic selection of polymeric carriers for ASDs.

The enhanced encapsulation, release, and oral hypoglycemic performance of a biomacromolecule surface modified insulin-loaded halloysite nanocomposite: an in vitro and in vivo study

To overcome the drawbacks of oral administration of insulin, a surface-modified insulin-loaded nanocomposite was designed and prepared in this work. Halloysite nanotubes (HNTs) were employed to improve the insulin encapsulation, PEG-CS and hydroxypropyl methyl cellulose phthalate (HPMCP) were selected to surface modify the insulin-loaded HNTs to adjust the release of insulin. As a result, the insulin-loaded HNTs/PEG-CS/HPMCP NCs had good biocompatibility, relatively high drug loading, and pH-sensitive release properties. Oral administration of the NCs produced an effective and relative long-time hypoglycemic effect. Therefore, these NCs can be a promising delivery system to improve the oral bioavailability of insulin.

Improved dissolution of an enteric polymer and its amorphous solid dispersions by polymer salt formation

Weakly acidic polymers, historically used as enteric coatings, are increasingly being employed in solubility-enhancing amorphous solid dispersion (ASD) formulations. However, there is a lack of fundamental understanding around how these carboxylic acid-containing polymers dissolve, in particular when molecularly mixed with a lipophilic drug, as in an ASD. Identification of critical factors dominating their dissolution is vital for rational design of new polymers with enhanced release properties to address contemporary ASD delivery challenges, notably achieving good release at higher drug loadings. Herein, after identification of polymer solubilization via ionization as the rate limiting step for dissolution, hydroxypropylmethyl cellulose phthalate (HP-50) was converted to a salt by neutralization of the phthalic acid groups with different bases. Surface normalized dissolution was performed to assess the dissolution rate improvement achieved by polymer pre-ionization via salt formation. Polymer salts showed ∼ 3-fold faster release than HP-50 at pH 6.8 (50 mM sodium phosphate buffer). Importantly, a polymer salt was able to maintain a rapid dissolution rate, irrespective of the buffer capacity of the medium, whereas the protonated polymer showed greatly diminished dissolution as medium buffer capacity decreased toward physiological gastrointestinal tract values. HP-50 and two polymer salts were formulated into ASDs with miconazole, a lipophilic and weakly basic antifungal drug, at a 20% drug loading. Rapid drug release rates were achieved with polymer salt ASDs, whereby drug release was 14 times faster than from the protonated HP-50 ASD. This study highlights the critical role of polymer ionization and buffer capacity in the dissolution of HP-50-based systems and how pre-ionization via polymer salt formation is a successful strategy for the design of new polymers for improved ASD performance.

Enteric-Coated Polymers Past and Present - A Review

Abstract: Tablet coating has evolved over the years, and today, there are various types of coating for the delayed release of a drug. Drugs can be enteric-coated to provide delayed release, protect the active pharmaceutical ingredients, minimize undesirable effects, and modify the pharmacokinetic properties of a drug, which will have clinical impacts. Certain types of drugs need to be enteric-coated for various reasons, such as gastric irritants or acid-liable drugs. This article will review ethylcellulose and polymethacrylate, their role in an enteric coating, and their process coating pa-rameters. Ethylcellulose can provide a short delayed release; it can be modified by adding pH-dependent polymers such as sodium alginate and hydroxypropyl methylcellulose phthalate for a long delayed release. On the other hand, polymethacrylate can also be employed to enteric coat drugs without additional polymers. Polymethacrylate, such as Eudragit®, comes in different grades with varying proportions of polymer ratio, allowing for targeted delayed drug release. These will impact which polymer to be employed. Upon choosing the coating material, modeling can also pre-dict in vitro and in vivo correlation as enteric-coated products can have unpredictable in vivo phar-macokinetic profiles. Today, the trend is moving away from the traditional coating, and towards new polymers, and with digitalization, there is a focus to start using data from laboratory experi-ments to be integrated with computational modeling, artificial intelligence, and machine learning to accurately predict key process parameters and film properties for high-quality products.

Combining enabling formulation strategies to generate supersaturated solutions of delamanid: In situ salt formation during amorphous solid dispersion fabrication for more robust release profiles

Poor solubility is a major challenge that can limit the oral bioavailability of many drugs, including delamanid, a weakly basic nitro-dihydro-imidazooxazole derivative used to treat tuberculosis. Amorphous solid dispersion (ASD) can improve the bioavailability of poorly water-soluble compounds, yet drug crystallization is a potential failure mechanism, particularly as the drug loading increases. The goal of the current study was two-fold: to enhance the stability of amorphous delamanid against crystallization and to improve drug release by developing ASDs containing the salt form of the drug. Various sulfonate salts of delamanid were prepared in amorphous form and evaluated for their tendency to crystallize and undergo chemical degradation following storage at 40 °C/75% relative humidity. Drug release was evaluated by a two-stage dissolution test consisting of an initial low pH stage, followed by transfer to a higher pH medium. For ASDs of the free base, small amounts of crystallinity during preparation were found to limit the drug release. Delamanid salts with sulfonic acids showed considerably improved amorphous stability. Tosylate, besylate, edisylate, and mesylate salts had high glass transition temperatures as well as good chemical and physical stability. In addition, a remarkable improvement in the drug release was observed when ASDs were prepared with these salts in comparison to the free base form. Specifically, ASDs with hydroxypropyl methylcellulose phthalate (HPMCP) at 25% drug loading exhibited near-complete drug release for all four sulfonate salts. These findings suggest that the dual strategy combining salt formation with ASD formation is a promising approach to alter the crystallization tendency and to improve drug release of problematic poorly water-soluble compounds.

Formulation and Characterization of Doxycycline-Loaded Polymeric Nanoparticles for Testing Antitumor/Antiangiogenic Action in Experimental Colon Cancer in Mice.

Nanotherapeutics can enhance the characteristics of drugs, such as rapid systemic clearance and systemic toxicities. Polymeric nanoparticles (PRNPs) depend on dispersion of a drug in an amorphous state in a polymer matrix. PRNPs are capable of delivering drugs and improving their safety. The primary goal of this study is to formulate doxycycline-loaded PRNPs by applying the nanoprecipitation method. Eudragit S100 (ES100) (for DOX-PRNP1) and hydroxypropyl methyl cellulose phthalate HP55 (for DOX-PRNP2) were tested as the drug carrying polymers and the DOX-PRNP2 showed better characteristics and drug release % and was hence selected to be tested in the biological study. Six different experimental groups were formed from sixty male albino mice. 1,2,-Dimethylhydrazine was used for 16 weeks to induce experimental colon cancer. We compared the oral administration of DOX-PRNP2 in doses of 5 and 10 mg/kg with the free drug. Results indicated that DOX-PRNP2 had greater antitumor activity, as evidenced by an improved histopathological picture for colon specimens as well as a decrease in the tumor scores. In addition, when compared to free DOX, the DOX-PRNP2 reduced the angiogenic indicators VEGD and CD31 to a greater extent. Collectively, the findings demonstrated that formulating DOX in PRNPs was useful in enhancing antitumor activity and can be used in other models of cancers to verify their efficacy and compatibility with our study.

Assessment of Exenatide loaded Biotinylated Trimethylated Chitosan/HP- 55 Nanoparticles.

Exenatide(EXE) is an anti-hyperglycemic agent approved for treating type 2 diabetes by the Food and Drug Administration(FDA). However, twice-daily injection of exenatide is inconvenient for most of the patients. In this study, biotinylated trimethylated chitosan(Bio-TMC) based nanoparticles were proposed to promote oral absorption of exenatide. Realizing the oral administration of exenatide is very important to alleviate patient suffering and improve patient compliance. Bio-TMC was synthesized, and the chemical structure was characterized by Fourier transform infrared (FT-IR) spectroscopy and 1H NMR spectroscopy. Nanoparticles were prepared through polyelectrolyte interaction in the presence of sodium Tripolyphosphate (TPP) and hydroxypropyl methylcellulose phthalate (HP-55). Formulations were physically and chemically characterized. In vitro release was investigated in different pH media. In vivo antidiabetic activities of biotin modified and non-biotin modified chitosan were evaluated in db/db mice. EXE-loaded Bio-TMC/HP-55 nanoparticles were spherical in shape with a mean diameter of 156.2 nm and zeta potential of +11.3 mV. The drug loading efficiency and loading content were 52.38% and 2.08%, respectively. In vitro release revealed that EXE-loaded Bio-TMC/HP-55 nanoparticles were released faster in pH 1.2 than pH 6.8 (63.71% VS 50.12%), indicating that nanoparticles have enteric characteristics. Antidiabetic activity study revealed that after oral administration to diabetic mice, the relative pharmacological bioavailability (FPharm%) of the biotin modified nanoparticles was found to be 1.27-fold higher compared to the unmodified ones, and the hypoglycemic effect was also found to be better. Bio-TMC/HP-55 nanoparticles are feasible as oral drug carriers of exenatide and have the potential to be extended to other drugs that are not readily oral, such as monoclonal antibodies, vaccines, genes, etc. These would be beneficial to the pharmaceutical industry. Further research will focus on the biodistribution of Bio-TMC/HP-55 nanoparticles after oral administration.

Formulation and evaluation of pH activated dosage form as minitablets in capsule for delivery of fesoterodine

ObjectivesIn the present study, an attempt is made to develop novel multifunctional sustained-release minitablets in a capsule system by film coating Fesoterodine for the treatment of urinary incontinence (increased urinating frequency). MethodologyThe direct compression technique was used to formulate the minitablets, and coating was applied using hydroxypropyl methylcellulose (HPMC) phthalate. The pre-formulation study was performed using tools like differential scanning calorimetry (DSC), infrared spectroscopy (IR) and post-formulation parameters such as hardness, thickness, weight variation, uniformity, and drug release. Drug release kinetics were studied for the formulations F1–F11. ResultsAll the pre- and post-formulation parameters were found to be within the limits. F1 and F2 result in burst release of the drug within 30 minutes. For the F3, F4, and F5 formulations, HPMC phthalate-coated minitablets show almost 100% drug release in 3, 4, and 5 hours, respectively. F6, F7, and F8 (2.5%, 5%, and 10% formaldehyde-coated minitablets, respectively) show drug releases in the small intestine, and the release was prolonged for 24 hours, whereas F9, F10, and F11 (2.5%, 5%, and 10% glutaraldehyde-coated minitablets, respectively) release in the small intestine, but drug release takes more than 20 hours. ConclusionFilm-coated minitablets were satisfactorily developed in terms of various post-compression parameters like hardness, thickness, friability, weight variation, and content uniformity. IR and DSC studies revealed no significant drug excipient interactions. HPMC phthalate-coated minitablets released in the buffer, and it was supposed that the drug releases in the intestine, which leads to better absorption and follows Korsmeyer-Peppas release kinetics.

Hydroxypropyl Methylcellulose Phthalate Biopolymer as an Anticorrosion Coating

Hydroxypropyl Methylcellulose Phthalate Biopolymer as an Anticorrosion Coating

Delayed sustained drug release from electrostatic powder coated tablets with ultrafine polymer blends

The present study aims to apply an electrostatic dry powder coating process to coat aspirin tablets with polymer blends to produce a single-layer coating film, which potentially allows an advantageous delayed sustained drug release profile. The coating formulations containing polymer blends of enteric polymer (hydroxypropyl methylcellulose phthalate or hydroxypropyl methyl cellulose acetate-succinate) and insoluble polymer (Eudragit® RL) were successfully developed and optimized. Results of scanning electron microscopy and acid resistance test demonstrated that curing conditions had a significant impact on the qualities of the produced film. Drug dissolution experiments revealed that changes in the coating level and the coating formulation with different ratios of the enteric polymer to the insoluble polymer achieved an altered and adjustable drug release profile. All of the results suggested that electrostatic powder coating technology is capable to produce a satisfactory coating film with polymer blends, allowing an advantageous functionality of delayed sustained drug release.