Encapsulation of antibiotics into nanocarriers has the potential to overcome resistance and disadvantages associated with conventional dosage forms as well as increase half-life of an antibiotic. Encapsulation of meropenem (MRPN) into solid lipid nanoparticles (SLNs) remains unexplored among the limited work reported on nanoformulation incorporating MRPN. The study aimed to use an experimental design, to optimize MRPN-loaded SLNs, and to undertake in vitro and in silico evaluations. A Box-Behnken design (BBD) was used to optimize manufacturing conditions of glycerol monostearate (GMS) SLNs loaded with MRPN. The SLNs were prepared using hot homogenization and ultrasonication method. Optimized MRPN-SLNs showed particle size, zeta potential, and entrapment efficiency of 112.61 ± 0.66 nm, −20.43 ± 0.99 mV, and 89.94 ± 1.26%, respectively. The morphology of the SLNs revealed nearly spherical shaped particles. Differential scanning calorimetry and X-ray diffraction analysis showed that meropenem was present in amorphous form in the SLNs. Controlled in vitro MRPN release from SLNs was achieved and followed the Korsmeyer-Peppas model (R2 = 0.9679). Prolonged in vitro antibacterial activity against Escherichia coli was also observed. The molecular modeling showed that both hydrophobic interactions and hydrogen bonding led to a stable MRPN-GMS complex formation, which was confirmed by its low heat of formation (−5536.13 kcal/mol). This stable complex could have contributed to the controlled release of MRPN from the SLNs and subsequent sustained antibacterial activity.
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Univ Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Shahid Sadoughi Univ Med Sci, Fac Pharm, Yazd, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Dara, Tahereh
Vatanara, Alireza
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Univ Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Vatanara, Alireza
Meybodi, Mohsen Nabi
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Shahid Sadoughi Univ Med Sci, Fac Pharm, Yazd, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Meybodi, Mohsen Nabi
Vakilinezhad, Molood Alsadat
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Univ Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Vakilinezhad, Molood Alsadat
Malvajerd, Soroor Sadegh
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Univ Tehran Med Sci, Fac Pharm, Nanotechnol Res Ctr, Tehran, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Malvajerd, Soroor Sadegh
Vakhshiteh, Faezeh
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Univ Tehran Med Sci, Fac Pharm, Nanotechnol Res Ctr, Tehran, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Vakhshiteh, Faezeh
Shamsian, Azam
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Univ Tehran Med Sci, Fac Pharm, Nanotechnol Res Ctr, Tehran, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Shamsian, Azam
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Sharifzadeh, Mohammad
Kaghazian, Hooman
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Pasteur Inst Iran, Dept Res & Dev, Tehran, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
Kaghazian, Hooman
Mosaddegh, Mohammad Hossein
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Shahid Sadoughi Univ Med Sci, Fac Pharm, Yazd, IranUniv Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran, Iran
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Gomal Univ, Fac Pharm, Dept Pharmaceut, Dera Ismail Khan 29050, Pakistan
Gomal Univ, Fac Pharm, Gomal Ctr Skin Regenerat Med & Drug Delivery Res, Dera Ismail Khan, Kpk, PakistanGomal Univ, Fac Pharm, Dept Pharmaceut, Dera Ismail Khan 29050, Pakistan
Khan, Kamran
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Shah, Shefaat Ullah
Althobaiti, Yusuf S.
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Taif Univ, Coll Pharm, Dept Pharmacol & Toxicol, Taif, Saudi Arabia
Taif Univ, Addict & Neurosci Res Unit, Taif, Saudi ArabiaGomal Univ, Fac Pharm, Dept Pharmaceut, Dera Ismail Khan 29050, Pakistan
Althobaiti, Yusuf S.
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Shah, Kifayat Ullah
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Ullah, Aman
Amin, Adnan
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Gomal Univ, Fac Pharm, Nat Prod Res Lab NPRL, Dera Ismail Khan, PakistanGomal Univ, Fac Pharm, Dept Pharmaceut, Dera Ismail Khan 29050, Pakistan
Amin, Adnan
Khan, Muhammad Khalid
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Gomal Univ, Fac Pharm, Dept Pharmaceut, Dera Ismail Khan 29050, PakistanGomal Univ, Fac Pharm, Dept Pharmaceut, Dera Ismail Khan 29050, Pakistan