紫杉醇两亲性共聚物纳米胶束体外释药动力学

采用低分子量PEG-PCL-PEG、mPEG-PLLA、mPEG-PDLLA等两亲性嵌段共聚物作载体包载紫杉醇形成纳米胶束.研究了不同载药率胶束在磷酸缓冲液中释放的动力学,发现紫杉醇PEG-PCL-PEG胶束和mPEG-PLLA胶束的体外释药遵从一级释放动力学;紫杉醇mPEG-PDLLA纳米胶束的体外释放多呈现出两段零级释放动力学;低载药率胶束表现出高释药率;体外释药过程中磷酸缓冲液的更新量越大,紫杉醇的释放率越高.     

Curcumin-loaded biodegradable polymeric micelles for colon cancer therapy in vitro and in vivo

Curcumin is an effective and safe anticancer agent, but its hydrophobicity inhibits its clinical application. Nanotechnology provides an effective method to improve the water solubility of hydrophobic drug. In this work, curcumin was encapsulated into monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles through a single-step nano-precipitation method, creating curcumin-loaded MPEG-PCL (Cur/MPEG-PCL) micelles. These Cur/MPEG-PCL micelles were monodisperse (PDI = 0.097 ± 0.011) with a mean particle size of 27.3 ± 1.3 nm, good re-solubility after freeze-drying, an encapsulation efficiency of 99.16 ± 1.02%, and drug loading of 12.95 ± 0.15%. Moreover, these micelles were prepared by a simple and reproducible procedure, making them potentially suitable for scale-up. Curcumin was molecularly dispersed in the PCL core of MPEG-PCL micelles, and could be slow-released in vitro. Encapsulation of curcumin in MPEG-PCL micelles improved the t(1/2) and AUC of curcumin in vivo. As well as free curcumin, Cur/MPEG-PCL micelles efficiently inhibited the angiogenesis on transgenic zebrafish model. In an alginate-encapsulated cancer cell assay, intravenous application of Cur/MPEG-PCL micelles more efficiently inhibited the tumor cell-induced angiogenesis in vivo than that of free curcumin. MPEG-PCL micelle-encapsulated curcumin maintained the cytotoxicity of curcumin on C-26 colon carcinoma cells in vitro. Intravenous application of Cur/MPEG-PCL micelle (25 mg kg(-1) curcumin) inhibited the growth of subcutaneous C-26 colon carcinoma in vivo (p < 0.01), and induced a stronger anticancer effect than that of free curcumin (p < 0.05). In conclusion, Cur/MPEG-PCL micelles are an excellent intravenously injectable aqueous formulation of curcumin; this formulation can inhibit the growth of colon carcinoma through inhibiting angiogenesis and directly killing cancer cells.     

A pH-triggered charge reversal and self-fluorescent micelle as a smart nanocarrier for doxorubicin controlled release

A novel pH-sensitive charge reversal and self-fluorescent polymeric micelle is designed and synthesized successfully. The smart micelle is prepared based on MPEG-polyurethane multi-block copolymer, which is synthesized by polycondensation, with 1, 4-bis (hydroxyethyl) piperazine (HEP) and hydroxyl-sulfamethazine (Hydroxyl-SM) as pH-sensitive molecules and fluorescein isothiocyanate (FITC) as fluorescent segment. The resulting MPEG-polyurethane multi-block copolymer is examined by ¹H–NMR, UV-vis spectra, fluorescence spectra and an acid-base titration. Moreover, the diameter, morphology and cytotoxicity of obtained polymer micelle are measured by dynamic light scattering (DLS), transmission electron microscopy (TEM) and MTT assay. The results indicate that the micelle has a small diameter of less than 200 nm and can remain unchanged within two weeks. Zeta-potential measurement shows that the negative charge of micelle can switch into positive charge as the pH value decreasing from 9.0 to 3.0. Subsequently, the fluorescence intensity decreases significantly with the reducing of pH values. The MTT assay shows the low cytotoxicity and good biocompatibility of the MPEG-polyurethane polymeric micelles. Finally, doxorubicin (DOX) is loaded into micelles to detect in vitro release behavior. The drug loaded micelles show a faster release behavior at pH 5.0 than that at pH 7.4. Therefore, the pH-sensitive charge reversal and self-fluorescent micelle can be a potential smart carrier for delivery and controlled release of protein drug.     

离子液体中ATRP合成MCC-g-PMAA及其分子对阿司匹林控释的应用

以离子液体氯化1-烯丙基-3-甲基咪唑（[Amim]Cl）为反应介质,利用原子转移自由基聚合（atom transfer radical polymerization,ATRP）法合成了微晶纤维素接枝有聚甲基丙烯酸（MCC-g-PMAA）的pH敏感性聚合物。用透析法将模型药物阿司匹林包覆在聚合物胶束内,并对载药胶束的体外药物释放机制进行研究。通过红外、核磁、透射电镜、X射线衍射和紫外分光光度计等分析手段对聚合物的结构、胶束形貌、胶束对阿司匹林的载药性能及释药性能进行了表征分析。结果表明：聚合物胶束能够在水溶液中自组装成球状胶束,对阿司匹林具有良好的包载效果,阿司匹林在碱性条件下的累积释放量大于酸性条件,载药胶束表现出了良好的pH敏感性和药物缓释性能。     

Non-enzymatic and enzymatic degradation of poly(ethylene glycol)-b-poly(?-caprolactone) diblock copolymer micelles in aqueous solution

The non-enzymatic and enzymatic degradation behaviors of the monomethoxy-poly(ethylene glycol)-b-poly(?-caprolactone) diblock copolymers (MPEG-PCL) micelles in aqueous solution were investigated by DLS, ¹H NMR, SEC and HPLC. It is found that the degradation mechanism of MPEG-PCL micelles in aqueous solution in non-enzymatic case is quite different from that in the presence of enzyme. In non-enzymatic case, the degradation induced by acidic catalysis was not found in low pH aqueous solution but the degradation of the micelles occurred under neutral and basic conditions. The degradation of MPEG-PCL micelles first happens near the interface region of the MPEG shell and PCL core, leading to the part detachment of PEG chains. With increasing degradation time, the degradation inside the PCL core with a random scission on PCL chains occurred. Compared with non-enzymatic degradation, the enzymatic degradation of MPEG-PCL micelles is much fast and the degradation rate of MPEG-PCL micelles is proportional to either the micelles or the enzyme concentration in a certain range. Based on the micelle degradation behaviors that we observed, a possible mechanism for the enzymatic degradation of the MPEG-b-PCL micelles including PCL core erosion which results in cavitization of micellar core and micellar dissociation is proposed.     

Thermosensitive biotinylated hydroxypropyl cellulose-based polymer micelles as a nano-carrier for cancer-targeted drug delivery

In this article, we report the synthesis of a novel amphiphilic hydroxypropyl cellulose-based polymer (HPC-PEG-Chol) that contained poly (ethylene glycol) and cholesterol-containing moieties with specific degrees of substitution. The resulting polymer was subsequently converted to a biotin conjugate (HPC-PEG-Chol-biotin), to develop a new potential cancer-targeted drug delivery system. The biotin conjugate was used to prepare micelles via the dialysis method. The polymeric micelles in aqueous solution presented a lower critical solution temperature (LCST) of 39.8 ^oC. The critical micelle concentration (CMC) values of the polymeric micelles at 25 and 45 °C were evaluated to be about 0.32 and 0. 25 g/L, respectively. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) analyses of the micelles revealed the spherical shapes of the micelles, with 84 nm mean diameters that increased with the increase of the temperature above LCST. The hydrophobic anticancer drug paclitaxel (PTX) was loaded in the micelles and the in vitro release behaviors of PTX were investigated at different temperatures. The release profile of PTX from the polymeric micelles revealed a thermosensitivity, since its release rate was higher at 41 °C than at 37 °C. Fluorescent microscopy analyses confirm that the PTX-loaded HPC-PEG-Chol-biotin is superior in cellular uptake, with very strong adsorption to both HeLa and MDA-MB-231 cancer cell lines. MTT assay in normal cells indicated that HPC-PEG-Chol-biotin micelles have great potential to be safely used in tumor-targeting chemotherapy.     

The structural,morphological and thermal properties of grafted pH-sensitive interpenetrating highly porous polymeric composites of sodium alginate/acrylic acid copolymers for controlled delivery of diclofenac potassium

In present investigation new formulations of Sodium Alginate/Acrylic acid hydrogels with high porous structure were synthesized by free radical polymerization technique for the controlled drug delivery of analgesic agent to colon. Many structural parameters like molecular weight between crosslinks (M_c), crosslink density (M_r), volume interaction parameter (v_2,s), Flory Huggins water interaction parameter and diffusion coefficient (Q) were calculated. Water uptake studies was conducted in different USP phosphate buffer solutions. All samples showed higher swelling ratio with increasing pH values because of ionization of carboxylic groups at higher pH values. Porosity and gel fraction of all the samples were calculated. New selected samples were loaded with the model drug (diclofenac potassium).The amount of drug loaded and released was determined and it was found that all the samples showed higher release of drug at higher pH values. Release of diclofenac potassium was found to be dependent on the ratio of sodium alginate/acrylic acid, EGDMA and pH of the medium. Experimental data was fitted to various model equations and corresponding parameters were calculated to study the release mechanism. The Structural, Morphological and Thermal Properties of interpenetrating hydrogels were studied by FTIR, XRD, DSC, and SEM.     

Engineering a drug eluting ocular patch for delivery and sustained release of anti-inflammatory therapeutics

Ocular inflammation is commonly associated with eye disease or injury. Effective and sustained ocular delivery of therapeutics remains a challenge due to the eye physiology and structural barriers. Herein, we engineered a photocrosslinkable adhesive patch (GelPatch) incorporated with micelles (MCs) loaded with loteprednol etabonate (LE) for delivery and sustained release of drug. The engineered drug loaded adhesive hydrogel, with controlled physical properties, provided a matrix with high adhesion to the ocular surfaces. The incorporation of MCs within the GelPatch enabled solubilization of LE and its sustained release within 15 days. In vitro studies showed that MC loaded GelPatch supported cell viability and growth. In addition, subcutaneous implantation of the MC loaded GelPatch in rats confirmed its in vivo biocompatibility and stability within 28 days. This non-invasive, adhesive, and biocompatible drug eluting patch can be used as a matrix for the delivery and sustained release of hydrophobic drugs.     

Fabrication of micelles from poly(butylene succinate) and poly(2‐methacryloyloxyethyl phosphorylcholine) copolymers as a potential drug carrier

A series of copolymers of poly(2‐methacryloyloxyethyl phosphorylcholine)‐b‐poly(butylene succinate)‐b‐poly(2‐methacryloyloxyethyl phosphorylcholine) (PMPC‐b‐PBS‐b‐PMPC) were synthesized by atom transfer radical polymerization. The structure of the polymers was characterized by ¹H NMR and infrared spectroscopy, and their thermal properties were described using TGA and DSC. In aqueous solutions, the PMPC‐b‐PBS‐b‐PMPC could form micelles with sizes ranging from 108 to 170 nm. In vitro release studies showed that acidic media and a longer PMPC chain benefited doxorubicin (DOX) release. 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assays indicated that the micelles had low cytotoxicity to HeLa and L929 cells. DOX‐loaded micelles exhibited high cytotoxicity to HeLa cells. Flow cytometry results demonstrated that DOX‐loaded micelles could be internalized by HeLa cells. The in vitro phagocytosis results showed 3.9‐fold and 5.5‐fold reductions compared with poly(lactic acid) (PLA) nanoparticles and PDS55 micelles. These results demonstrate that PMPC‐b‐PBS‐b‐PMPC block copolymer micelles have great promise for cancer therapy. © 2017 Society of Chemical Industry     

载阿奇霉素-鼠李糖脂胶束制备工艺优化及性能表征

采用薄膜水化法制备载阿奇霉素-鼠李糖脂(AZI-RHL)胶束,以包封率、载药量为评价指标,通过单因素试验和正交试验优化制备工艺,并考察其理化性质。制备载药胶束前先测定RHL水溶液的临界胶束浓度(CMC)。结果表明,RHL水溶液的CMC值约为0.25 mg/mL。优化后的最佳制备工艺条件为：RHL投料量100 mg,甲醇用量12 mL,搅拌时长20 min。在此条件下制备的AZI-RHL胶束呈球形,水动力学直径为136.3±68.5 nm,Zeta电位为-23.1±6.8 mV,包封率为80.34%±0.60%,载药量为19.42%±0.48%。红外光谱证明AZI包埋在胶束中。体外释放试验表明AZI-RHL胶束具有一定的缓释作用,其体外累计释放曲线符合Ritger-Peppas方程,释放药物以Fick扩散为主。综上所述,AZI-RHL胶束的制备工艺稳定可靠,胶束粒径小,且包封率、载药量高,是一种有潜力的新型制剂。     

Treating colon cancer with a suicide gene delivered by self-assembled cationic MPEG-PCL micelles

Biodegradable cationic micelles show promise for applications in gene delivery. In this article, we used DOTAP to modify monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL, MP) micelles in one step, creating novel cationic self-assembled DOTAP and MPEG-PCL hybrid micelles (DMP). These micelles had a mean particle size of 46 ± 5.6 nm and a zeta potential of 41.8 ± 0.5 mV, and had the capacity to bind DNA. Compared with PEI25K (the gold standard), DMP micelles had higher transfection efficiency and lower cytotoxicity. Moreover, we used DMP to deliver the Survivin-T34A gene (S-T34A, a suicide gene) to treat colon cancer. DMP delivered the Survivin-T34A gene (DMP/S-T34A) and could induce apoptosis in cancer cells, resulting in inhibition of the growth of C-26 colon cancer cells in vitro. An in vivo study indicated that intraperitoneal administration of DMP micelles delivered the Survivin-T34A gene and efficiently inhibited the growth of abdominal metastatic C-26 colon cancer and the malignant ascites. These data suggest that DMP may be a novel gene carrier, and its delivery of the S-T34A gene may have promising applications in the treatment of colon cancer.     

Influence of structure on release profile of acyclovir loaded polyurethane nanofibers: Monolithic and core/shell structures

In this study, monolithic and core/shell polyurethane (PU) nanofibers were fabricated by single and coaxial electrospinning techniques, respectively. An antivirus drug, Acyclovir (ACY), was loaded on PU nanofibers. The physical condition and interaction of the loaded ACY within these nanofibers were studied by FTIR, XRD, DSC, SEM, and TEM. In vitro tests exhibited an obvious difference in the release pattern between monolithic and core/shell nanofibers and burst release in monolithic nanofibers could be controlled by core/shell structure. Release profile was found to follow Korsmeyere‐Peppas model with Fickian diffusion mechanism. Our study demonstrated that the ACY‐loaded core/shell nanofibers might serve as a device for drug delivery systems. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 44073.     

Biodegradable polylactide/poly(ethylene glycol)/polylactide triblock copolymer micelles as anticancer drug carriers

Adriamycin (ADR) was selected as a model drug to evaluate the potential applications of polylactide/poly(ethylene glycol)/polylactide (PLA/PEG/PLA) micelles as drug carriers in parenteral delivery systems. The PLA/PEG/PLA triblock copolymer micelles were characterized by dynamic light scattering and transmission electron microscopy. It was found that the micelle size increased with the increasing of the PLA chain length. The average size of ADR‐loaded micelles was 143.2 nm. The histogram analysis showed that the ADR‐loaded micelles possessed a narrow unimodal size distribution. The ADR loading contents of the micelles and ADR entrapment efficiency were dependent on the PLA chain length and PEG chain length in the copolymer. They increased with the increase of the PLA chain length, but the PEG chain length was identical and decreased with the increase of the PEG chain length; the length of the PLA block was similar. The initial amount of ADR also influenced the drug contents and entrapment efficiency (i.e., the more the initial amount added, the more the drug contents and the higher encapsulation efficiency). The drug release experiments indicated that the ADR‐loaded micelles possessed sustained release characteristics. © 2001 John Wiley & Sons, Inc. J Appl Polym Sci 80: 1976–1982, 2001     

Biodegradable depsipeptide–PDO–PEG-based block copolymer micelles as nanocarriers for controlled release of doxorubicin

Nowadays, biodegradable amphiphilic block copolymers with stable performance and adjustable structure have attracted the interests of researchers in the field of drug delivery. In this work, the triblock copolymer, P(SBMD-co-PDO)-b-PEG-b-P(SBMD-co-PDO), was successfully synthesized by ring-opening polymerization of 3(S)-sec-butyl-morpholine-2,5-dione (SBMD) and p-dioxanone (PDO) with poly(ethylene glycol) (PEG) as the initiator. In phosphate buffered solution (PBS), these copolymers could self-assemble into nano-sized micelles that have a hydrophobic P(SBMD-co-PDO) core surrounded by a hydrophilic PEG shell. Because of the strong hydrogen bonding and hydrophobic interactions, doxorubicin (DOX) was loaded into the micelles with high loading capacity (LC, up to 28.4%) and encapsulation efficiency (EE, up to 62.5%). The drug-loaded micelles showed sustained-release of DOX along with the hydrolytic degradation of the micelles in PBS. Therefore, these amphiphilic triblock copolymers have potential as drug matrix for controlled release.     

Improving anti-tumor activity with polymeric micelles entrapping paclitaxel in pulmonary carcinoma

Nanoscale polymeric micelles have promising applications as drug delivery systems (DDS). In this work, to improve the anti-tumor activity and eliminate toxicity of the commercial formulation (cremophor EL and ethanol) of paclitaxel (PTX), we developed biodegradable poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles entrapping PTX by a simple one-step solid dispersion method, which is without any surfactants or additives and is easy to scale up. In addition, the PTX micelles could be lyophilized into powder without any adjuvant and the re-dissolved PTX micelles are stable and homogeneous. The prepared PTX micelles have a mean particle size of 38.06 ± 2.30 nm, a polydispersity index of 0.168 ± 0.014, a drug loading of 14.89 ± 0.06% and an encapsulation efficiency of 99.25 ± 0.38%. A molecular modeling study implied that PTX interacted with PCL as a core, which was embraced by PEG as a shell. The encapsulation of PTX in polymeric micelles enhanced its cytotoxicity by increasing the uptake by LL/2 cells. A sustained in vitro release behavior and slow extravasation behavior from blood vessels in a transgenic zebrafish model were observed in the PTX micelles. Furthermore, compared with Taxol?, the PTX micelles were more effective in suppressing tumor growth in the subcutaneous LL/2 tumor model. The PTX micelles also inhibited metastases in the pulmonary metastatic LL/2 tumor model and prolonged survival in both mouse models. Pharmacokinetic and tissue distribution studies showed that after PTX was encapsulated in polymeric micelles, the biodistribution pattern of PTX was altered and the PTX concentration in tumors was increased compared with Taxol? after intravenous injection. In conclusion, we have developed a polymeric micelles entrapping PTX that enhanced cytotoxicity in vitro and improved anti-tumor activity in vivo with low systemic toxicity on pulmonary carcinoma. The biodegradable MPEG-PCL micelles entrapping PTX may have promising applications in pulmonary carcinoma therapy.     

Core/shell pH‐sensitive micelles self‐assembled from cholesterol conjugated oligopeptides for anticancer drug delivery

A doxorubicin (DOX) delivery system of pH‐sensitive micelles self‐assembled from cholesterol conjugated His₅Arg₁₀ (HR15‐Chol) and His₁₀Arg₁₀ (HR20‐Chol) has been described in this article. The amphiphilic molecules have low critical micelle concentrations of 17.8 and 28.2 μg/mL for HR15‐Chol and HR20‐Chol, respectively, even at a low pH of 5.0. The pH‐sensitive histidine segment of the polypeptide block is insoluble at pH 7.4 but becomes positively charged and soluble via protonation at pH lower than 6.0. The size and zeta potential of DOX‐loaded micelles increases with the decrease in pH. Coarse‐grained simulations were performed to verify the structure of DOX‐loaded micelles and pH sensitivity of HR15/20‐Chol. The in vitro DOX release from the micelles is significantly accelerated by decreasing pH from 7.4 to 5.0. Furthermore, DOX release from the micelles is controlled by a Fickian diffusion mechanism. These micelles have great potential applications in delivering hydrophobic anticancer drugs for improved cancer therapy. © 2009 American Institute of Chemical Engineers AIChE J, 2010     

Micelles formed by self‐assembly of hyperbranched poly[(amine‐ester)‐co‐(D,L‐lactide)] (HPAE‐co‐PLA) copolymers for protein drug delivery

BACKGROUND: The aim of the work presented was to synthesize a series of amphiphilic hyperbranched poly[(amine‐ester)‐co‐(D ,L ‐lactide)] (HPAE‐co‐PLA) copolymers and study the formation of copolymeric micelles. These copolymeric micelle systems are expected to be potential candidates for applications in protein drug delivery. RESULTS: The chemical structures of the copolymers were confirmed by Fourier transform infrared spectroscopy, ¹³C NMR and thermogravimetric analysis. Fluorescence spectroscopy and dynamic light scattering confirmed the formation of copolymeric micelles of the HPAE‐co‐PLA copolymers. The maintenance of stability of bovine serum albumin (BSA) during release from micelles in vitro was also measured using circular dichroism and fluorescence spectrometry. CONCLUSION: Novel hyperbranched HPAE‐co‐PLA copolymers have been synthesized. Conjugation of PLA to HPAE was proved to be an available method for the preparation of micelles for protein delivery. The BSA‐loaded micelles showed enhanced encapsulation efficiency and the structural stability of BSA was retained during the release process. The hyperbranched polymeric micelles could be useful as drug carriers for protein drug delivery systems. Copyright © 2008 Society of Chemical Industry     

Synthesis and characterization of PEG–PCL–PEG triblock copolymers as carriers of doxorubicin for the treatment of breast cancer

Triblock copolymers of monomethoxy poly(ethylene glycol) (mPEG) and ε‐caprolactone (CL) were prepared with varying lengths of poly(ε‐caprolactone) (PCL) compositions and a fixed length of mPEG segment. The molecular characteristics of triblock copolymers were characterized by ¹H NMR, gel permeation chromatography (GPC), Fourier transform infrared spectroscopy (FT‐IR), X‐ray diffraction (XRD), and differential scanning calorimetry (DSC). These amphiphilic linear copolymers based on PCL hydrophobic chain and hydrophilic mPEG ending, which can self‐assemble into nanoscopic micelles with their hydrophobic cores, encapsulated doxorubicin (DOX) in an aqueous solution. The particle size of prepared micelles was around 40–92 nm. The DOX loading content and DOX loading efficiency were from 3.7–7.4% to 26–49%, respectively. DOX‐released profile was pH‐dependent and faster at pH 5.4 than pH 7.4. Additionally, the cytotoxicity of DOX‐loaded micelles was found to be similar with free DOX in drug‐resistant cells (MCF‐7/adr). The great amounts of DOX and fast uptake accumulated into the MCF‐7/adr cells from DOX‐loaded micelles suggest a potential application in cancer chemotherapy. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010     

Evaluation of micellar architecture based on functionalized chitosan for the in vitro release of an antibiotic

Polymeric micelles are enjoying high resurgence of interest in biomedical field as promising candidates for the delivery of water-insoluble drugs. This property was used to design and synthesize fatty acid grafted polysaccharide-based copolymer micelles for the sustained release of Cefixime trihydrate (CFX): a third-generation cephalosporin. Chitosan (CS), a polysaccharide obtained by the alkaline deacetylation of chitin emerged as a useful drug delivery matrix because of its polycationic nature, biodegradability, biocompatibility and mucoadhesiveness. The drug release was monitored in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (7.4). The in vitro release studies revealed 52% of drug release after 24 h of incubation and were enhanced to 83% after 72 h in simulated intestinal fluid condition. Antibacterial studies confirmed that the inherent properties of the drug were retained as well as enhanced by micelle formation. Thus, the synthesized copolymer micelle assures to be an excellent carrier vehicle for the sustained release of a model hydrophobic drug CFX. Smaller particle size ensures increased drug uptake and controlled release facilitates patient compliance.     

Development of sericin/alginate particles by ionic gelation technique for the controlled release of diclofenac sodium

Sericin and alginate particles, prepared by ionic gelation technique, demonstrated to be a promising matrix to controlled release of diclofenac sodium. Ten particle compositions of sericin, alginate, and diclofenac were evaluated. The drug incorporation was confirmed by scanning electron microscopy, Fourier Transform Infrared Spectroscopy, and X‐ray diffraction analysis. In vitro dissolution profile was performed to obtain the drug release profile in gastric and enteric medium. The drug release profile indicated that sericin delays the release and alginate contributes to the gastro‐resistance of formulations. The blend with composition of 2.5% of sericin, 2.8% of alginate with 2.0% w/v of diclofenac demonstrated to be feasible for drug delivery due the entrapment efficiency of 81.06% and release delay of 360 min, the highest time of all investigated compositions. The mathematical modeling showed that the drug release mechanism is associated to the process of swelling, matrix erosion, and a combination of diffusion and chain relaxation mechanisms. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 45919.